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1. Full Text Discovery of a Clinical Stage Multi-Kinase Inhibitor Sodium (E)-2-{2-Methoxy-5-[(2′,4′,6′-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): Synthesis, Structure–Activity Relationship, and Biological Activity
by Reddy, M. V. Ramana and Venkatapuram, Padmavathi and Mallireddigari, Muralidhar R and Pallela, Venkat R and Cosenza, Stephen C and Robell, Kimberly A and Akula, Balaiah and Hoffman, Benjamin S and Reddy, E. Premkumar
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2011, Volume 54, Issue 18, pp. 6254 - 6276
Cyclin D proteins are elevated in many cancer cells, and targeted deletion of cyclin D1 gene in the mammary tissues protects mice from breast cancer.... 
OXIDATION | CHEMISTRY, MEDICINAL | AGENTS | LEUKEMIA | DERIVATIVES | Glycine - analogs & derivatives | Neoplasm Transplantation | Drug Resistance, Multiple | Stereoisomerism | Antineoplastic Agents - chemical synthesis | Humans | Biological Availability | Drug Resistance, Neoplasm | Transplantation, Heterologous | Structure-Activity Relationship | Sulfones - pharmacology | Protein Kinase Inhibitors - chemistry | Glycine - chemistry | Sulfones - chemistry | Female | Antineoplastic Agents - pharmacology | Sulfones - chemical synthesis | Protein Kinase Inhibitors - chemical synthesis | Antineoplastic Agents - chemistry | Animals | Glycine - chemical synthesis | Glycine - pharmacology | Mice, Nude | Cell Line, Tumor | Mice | Protein Kinase Inhibitors - pharmacology | Apoptosis | Drug Screening Assays, Antitumor
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2. Full Text Synthesis of hetero annulated isoxazolo-, pyrido- and pyrimido carbazoles: Screened for in vitro antitumor activity and structure activity relationships, a novel 2-amino-4-(3'-bromo-4'-methoxyphenyl)-8-chloro-11H-pyrimido[4,5-a]carbazole as an antitumor agent
by Murali, Karunanidhi and Sparkes, Hazel A and Rajendra Prasad, Karnam Jayarampillai
European Journal of Medicinal Chemistry, ISSN 0223-5234, 03/2017, Volume 128, pp. 319 - 331
Claisen-Schmidt condensation of 2,3,4,9-tetrahydro-1 -carbazol-1-one with 3-bromo-4-methoxy benzaldehyde afforded the... 
Hetero annulated carbazoles | Pyrimidocarbazole | Cytotoxicity | Fluorescent microscopic analysis | Structure-activity relationship | LUNG-CANCER | POTENT | CHEMISTRY, MEDICINAL | ANTIOXIDANT | BIOLOGICAL EVALUATION | DERIVATIVES | Pyrimidines - chemical synthesis | Humans | Carbazoles - chemical synthesis | Structure-Activity Relationship | Isoxazoles - chemistry | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Spectroscopy, Fourier Transform Infrared | Pyrimidinones - chemistry | Neoplasms - drug therapy | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Molecular Structure | Pyridones - chemistry | Tumor Cells, Cultured | Carbazoles - pharmacology | Neoplasms - pathology | Drug Screening Assays, Antitumor | Antimitotic agents | Hydroxides | Antineoplastic agents | Analysis | Nitriles
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3. Full Text Structure−activity relationships of 2‑quinolinecarboxaldehyde thiosemicarbazone gallium(III) complexes with potent and selective anticancer activity
by Cao, Wanbao and Qi, Jinxu and Qian, Kun and Tian, Liang and Cheng, Zhen and Wang, Yihong
Journal of Inorganic Biochemistry, ISSN 0162-0134, 02/2019, Volume 191, pp. 174 - 182
Six gallium(III) complexes (Ga1–Ga6) with 2‑quinolinecarboxaldehyde thiosemicarbazone analogues were synthesized and characterized. These gallium(III)... 
Gallium(III) complex | 2‑Quinolinecarboxaldehyde thiosemicarbazone | Metallodrugs | Anticancer activity | CANCER-CELLS | APOPTOSIS | ANTIPROLIFERATIVE ACTIVITY | 2-Quinolinecarboxaldehyde thiosemicarbazone | BIOCHEMISTRY & MOLECULAR BIOLOGY | CASPASE-3 | INDUCTION | ANTITUMOR-ACTIVITY | CELLULAR UPTAKE | CHEMISTRY, INORGANIC & NUCLEAR | DI-2-PYRIDYLKETONE | GA(III) | EXPRESSION
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4. Full Text Activity-Based Proteome Profiling of Potential Cellular Targets of Orlistat − An FDA-Approved Drug with Anti-Tumor Activities
by Yang, Peng-Yu and Liu, Kai and Ngai, Mun Hong and Lear, Martin J and Wenk, Markus R and Yao, Shao Q
Journal of the American Chemical Society, ISSN 0002-7863, 01/2010, Volume 132, Issue 2, pp. 656 - 666
Orlistat, or tetrahydrolipstatin (THL), is an FDA-approved antiobesity drug with potential antitumor activities. Cellular off-targets and potential side... 
TISSUE SAMPLES | HER-2/NEU ERBB-2 | VIRULENCE FACTORS | PROSTATE-CANCER | ANTIOBESITY DRUG | BETA-LACTONES | FATTY-ACID SYNTHASE | INHIBITORS | IDENTIFICATION | CHEMISTRY, MULTIDISCIPLINARY | THIOESTERASE DOMAIN | United States | Humans | Molecular Conformation | Molecular Probes - pharmacology | Structure-Activity Relationship | Molecular Probes - chemical synthesis | Antineoplastic Agents - chemistry | Lactones - metabolism | Proteome - chemistry | Lactones - pharmacology | Antineoplastic Agents - metabolism | Dose-Response Relationship, Drug | Lactones - chemical synthesis | Molecular Probes - chemistry | Drug Design | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Tumor Cells, Cultured | Proteome - metabolism | United States Food and Drug Administration | Drug Screening Assays, Antitumor | Lactones - chemistry | Usage | Care and treatment | Gene mutations | Western immunoblotting | Analysis | Proteomics | Orlistat | Chemical properties | Research | Health aspects | Cancer | Index Medicus
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5. Full Text Design, synthesis, topoisomerase I & II inhibitory activity, antiproliferative activity, and structure–activity relationship study of pyrazoline derivatives: An ATP-competitive human topoisomerase IIα catalytic inhibitor
by Ahmad, Pervez and Woo, Hyunjung and Jun, Kyu-Yeon and Kadi, Adnan A and Abdel-Aziz, Hatem A and Kwon, Youngjoo and Rahman, A.F.M. Motiur
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 04/2016, Volume 24, Issue 8, pp. 1898 - 1908
A series of pyrazoline derivatives ( ) were synthesized in 92–96% yields from chalcones ( ) and hydrazides ( ). Subsequently, topo-I and IIα-mediated... 
Topoisomerase | Pyrazoline derivatives | ATP-competitive inhibitor | Antiproliferative activity | CHEMISTRY, MEDICINAL | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHROMENOPYRIDINES | CHEMISTRY, ORGANIC | ANTIAMEBIC ACTIVITY | SULFONAMIDE | DISCOVERY | ANTITUMOR EVALUATION | POTENT | ANTICANCER | BIOLOGICAL EVALUATION | OPTIMIZATION | CYTOTOXICITY | Pyrazoles - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Structure-Activity Relationship | DNA-Binding Proteins - metabolism | Dose-Response Relationship, Drug | Topoisomerase Inhibitors - pharmacology | Topoisomerase Inhibitors - chemical synthesis | Pyrazoles - chemistry | Biocatalysis - drug effects | Adenosine Triphosphate - metabolism | Drug Design | Antigens, Neoplasm - metabolism | Antineoplastic Agents - pharmacology | Molecular Structure | Pyrazoles - pharmacology | Cell Survival - drug effects | DNA Topoisomerases, Type II - metabolism | DNA-Binding Proteins - antagonists & inhibitors | DNA Topoisomerases, Type I - metabolism | Antineoplastic Agents - chemistry | Binding, Competitive - drug effects | Cell Line, Tumor | Cell Proliferation - drug effects | Molecular Docking Simulation | Topoisomerase Inhibitors - chemistry | Drug Screening Assays, Antitumor
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6. Full Text Design, synthesis and structure–activity relationship of phthalimides endowed with dual antiproliferative and immunomodulatory activities
by Cardoso, Marcos Veríssimo de Oliveira and Moreira, Diogo Rodrigo Magalhães and Filho, Gevanio Bezerra Oliveira and Cavalcanti, Suellen Melo Tiburcio and Coelho, Lucas Cunha Duarte and Espíndola, José Wanderlan Pontes and Gonzalez, Laura Rubio and Rabello, Marcelo Montenegro and Hernandes, Marcelo Zaldini and Ferreira, Paulo Michel Pinheiro and Pessoa, Cláudia and Alberto de Simone, Carlos and Guimarães, Elisalva Teixeira and Soares, Milena Botelho Pereira and Leite, Ana Cristina Lima
European Journal of Medicinal Chemistry, ISSN 0223-5234, 05/2015, Volume 96, pp. 491 - 503
The present work reports the synthesis and evaluation of the antitumour and immunomodulatory properties of new phthalimides derivatives designed to explore... 
Antiproliferative | Immunosuppressive | Phthalimide | Thiosemicarbazone | Thiazolidinone | Thiazole | MULTIPLE-MYELOMA | KAPPA-B KINASE | ANTIINFLAMMATORY ACTIVITY | CHEMISTRY, MEDICINAL | TRANSITION-METAL COMPLEXES | CARCINOMA-CELL LINES | FACTOR-ALPHA | TUMOR-NECROSIS-FACTOR | INTERFERON-GAMMA | THALIDOMIDE ANALOGS | INHIBITORS | Immunomodulation | Antineoplastic Agents - chemical synthesis | Cytokines - analysis | Humans | Cells, Cultured | Models, Molecular | Crystallography, X-Ray | Male | Phthalimides - chemistry | Structure-Activity Relationship | Antineoplastic Agents - chemistry | Dose-Response Relationship, Drug | Phthalimides - pharmacology | Animals | Phthalimides - chemical synthesis | Lymphocytes - drug effects | Drug Design | Macrophages - drug effects | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Mice | Mice, Inbred BALB C | Molecular Structure | Drug Screening Assays, Antitumor | Prevention | Cancer
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7. Full Text Substituted 4‑(Thiazol-5-yl)-2-(phenylamino)pyrimidines Are Highly Active CDK9 Inhibitors: Synthesis, X‑ray Crystal Structures, Structure–Activity Relationship, and Anticancer Activities
by Shao, Hao and Shi, Shenhua and Huang, Shiliang and Hole, Alison J and Abbas, Abdullahi Y and Baumli, Sonja and Liu, Xiangrui and Lam, Frankie and Foley, David W and Fischer, Peter M and Noble, Martin and Endicott, Jane A and Pepper, Chris and Wang, Shudong
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2013, Volume 56, Issue 3, pp. 640 - 659
Cancer cells often have a high demand for antiapoptotic proteins in order to resist programmed cell death. CDK9 inhibition selectively targets survival... 
IN-VITRO | CHEMISTRY, MEDICINAL | R-ROSCOVITINE | MCL-1 EXPRESSION | DRUG DESIGN | CHRONIC LYMPHOCYTIC-LEUKEMIA | POTENT CLASS | CELL-CYCLE | DEPENDENT KINASE INHIBITOR | STRUCTURE-BASED DESIGN | P-TEFB | Protein Kinase Inhibitors - chemical synthesis | Magnetic Resonance Spectroscopy | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Models, Molecular | Crystallography, X-Ray | Cyclin-Dependent Kinase 9 - antagonists & inhibitors | Structure-Activity Relationship | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Pyrimidines - chemistry | Protein Kinase Inhibitors - chemistry | Spectrometry, Mass, Electrospray Ionization | Cell Line, Tumor | Antineoplastic Agents - pharmacology | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Drug Screening Assays, Antitumor | Antitumor activity
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8. Full Text Synthesis, anticancer and antioxidant activities of 2,4,5-trimethoxy chalcones and analogues from asaronaldehyde: Structure–activity relationship
by Shenvi, Suvarna and Kumar, Krishna and Hatti, Kaushik S and Rijesh, K and Diwakar, Latha and Reddy, G. Chandrasekara
European Journal of Medicinal Chemistry, ISSN 0223-5234, 04/2013, Volume 62, pp. 435 - 442
2,4,5-Trimethoxy chalcones and analogues were synthesized from asaronaldehyde derived from β-asarone. These novel compounds when tested against three human... 
Flavonols | Chalcones | In-silico | Flavones | Antioxidant | Anticancer | GROWTH-INHIBITION | DESIGN | CHEMISTRY, MEDICINAL | FLAVONOIDS | METHOXYLATED CHALCONES | BIOLOGICAL EVALUATION | CELL-CYCLE | DERIVATIVES | Cell Survival - drug effects | Chalcones - chemistry | Antioxidants - chemistry | Antineoplastic Agents - chemical synthesis | Humans | Structure-Activity Relationship | Antioxidants - chemical synthesis | Antioxidants - pharmacology | Antineoplastic Agents - chemistry | Dose-Response Relationship, Drug | Chalcones - chemical synthesis | MCF-7 Cells | Chalcones - pharmacology | Cell Line, Tumor | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Molecular Structure | Cell Death - drug effects | HeLa Cells | Aldehydes - chemistry | Drug Screening Assays, Antitumor | Antioxidants | Care and treatment | Hydrazine | Analysis | Cancer | Flavonoids | Bioflavonoids
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9. Full Text Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities
by Akhtar, Jawaid and Khan, Ahsan Ahmed and Ali, Zulphikar and Haider, Rafi and Shahar Yar, M
European Journal of Medicinal Chemistry, ISSN 0223-5234, 01/2017, Volume 125, pp. 143 - 189
The present review article offers a detailed account of the design strategies employed for the synthesis of nitrogen-containing anticancer agents. The results... 
SARs | N-Heterocycles | Anticancer | Cytotoxic | ANTIPROLIFERATIVE ACTIVITY | DNA-BINDING | CHEMISTRY, MEDICINAL | HIGHLY SELECTIVE LIGANDS | IN-VITRO EVALUATION | POTENTIAL ANTITUMOR | BIOLOGICAL EVALUATION | AGENTS DESIGN | HISTONE DEACETYLASE INHIBITORS | ANTITUMOR-ACTIVITY EVALUATION | PHARMACOLOGICAL EVALUATION | Nitrogen Compounds - pharmacology | Heterocyclic Compounds - chemistry | Humans | Nitrogen Compounds - chemistry | Drug Design | Heterocyclic Compounds - pharmacology | Antineoplastic Agents - pharmacology | Structure-Activity Relationship | Antineoplastic Agents - chemistry | Pyrimidines | Care and treatment | Pyridine | Protein kinases | Analysis | Cancer
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10. Full Text Synthesis and Quantitative Structure–Activity Relationship of Imidazotetrazine Prodrugs with Activity Independent of O6‑Methylguanine-DNA-methyltransferase, DNA Mismatch Repair, and p53
by Pletsas, Dimitrios and Garelnabi, Elrashied A. E and Li, Li and Phillips, Roger M and Wheelhouse, Richard T
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2013, Volume 56, Issue 17, pp. 7120 - 7132
The antitumor prodrug temozolomide is compromised by its dependence for activity on DNA mismatch repair (MMR) and the repair of the chemosensitive DNA lesion,... 
THERAPY-RELATED CANCER | ANTITUMOR DRUG TEMOZOLOMIDE | IN-VITRO | CHEMISTRY, MEDICINAL | METHYLATING AGENTS | METHYLTRANSFERASE | MECHANISM | DISCOVERY SCREEN | DECOMPOSITION | ALKYLTRANSFERASE | MITOZOLOMIDE | O-Methylguanine-DNA Methyltransferase - chemistry | Base Pair Mismatch | Prodrugs - chemistry | DNA Repair | Quantitative Structure-Activity Relationship | Tumor Suppressor Protein p53 - metabolism
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11. Full Text Potent, Orally Active Heterocycle-Based Combretastatin A-4 Analogues:  Synthesis, Structure−Activity Relationship, Pharmacokinetics, and In Vivo Antitumor Activity Evaluation
by Wang, Le and Woods, Keith W and Li, Qun and Barr, Kenneth J and McCroskey, Richard W and Hannick, Steven M and Gherke, Laura and Credo, R. Bruce and Hui, Yu-Hua and Marsh, Kennan and Warner, Robert and Lee, Jang Y and Zielinski-Mozng, Nicolette and Frost, David and Rosenberg, Saul H and Sham, Hing L
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2002, Volume 45, Issue 8, pp. 1697 - 1711
The synthesis and structure−activity relationship study of a series of compounds with heterocycles in place of the cis double bond in combretastatin A-4 (CA-4)... 
CHEMISTRY, MEDICINAL | ASYMMETRIC-SYNTHESIS | PRODRUG | ANTIMITOTIC AGENTS | RESISTANCE | CELL-LINES | TUBULIN | CYTOTOXICITY | DERIVATIVES | INDOLES | Neoplasm Transplantation | Antineoplastic Agents - chemical synthesis | Humans | Imidazoles - chemistry | Transplantation, Heterologous | Stilbenes - chemistry | Structure-Activity Relationship | Imidazoles - pharmacokinetics | Biopolymers | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Imidazoles - chemical synthesis | Tubulin - chemistry | Tumor Cells, Cultured | Lymphoma, Large B-Cell, Diffuse - drug therapy | Lymphoma, Large B-Cell, Diffuse - pathology | Administration, Oral | Rats | Imidazoles - pharmacology | Antineoplastic Agents - chemistry | Cell Division - drug effects | Haplorhini | Animals | Mice, Nude | Dogs | Mice | Drug Screening Assays, Antitumor
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12. Full Text Antimitotic and Antiproliferative Activities of Chalcones: Forward Structure–Activity Relationship
by Boumendjel, Ahcène and Boccard, Julien and Carrupt, Pierre-Alain and Nicolle, Edwige and Blanc, Madeleine and Geze, Annabelle and Choisnard, Luc and Wouessidjewe, Denis and Matera, Eva-Laure and Dumontet, Charles
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2008, Volume 51, Issue 7, pp. 2307 - 2310
A series of 59 chalcones was prepared and evaluated for the antimitotic effect against K562 leukemia cells. The most active chalcones were evaluated for their... 
CHEMISTRY, MEDICINAL | ANALOGS | BIOLOGICAL EVALUATION | AGENTS | FLAVONOIDS | BINDING | DISCOVERY | Cell Survival - drug effects | Chalcones - chemistry | Antimitotic Agents - toxicity | Stereoisomerism | Humans | Survival Rate | Structure-Activity Relationship | Antineoplastic Agents - chemistry | Antineoplastic Agents - toxicity | Animals | Chalcones - toxicity | Drug-Related Side Effects and Adverse Reactions | Chalcones - pharmacology | Cell Line, Tumor | Antimitotic Agents - pharmacology | Antineoplastic Agents - pharmacology | Cell Proliferation - drug effects | Mice | Molecular Structure | Cell Cycle - drug effects | Antimitotic Agents - chemistry | Drug Screening Assays, Antitumor | Index Medicus
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13. Full Text Novel Potent Orally Active Selective VEGFR-2 Tyrosine Kinase Inhibitors:  Synthesis, Structure−Activity Relationships, and Antitumor Activities of N-Phenyl-N‘-{4-(4-quinolyloxy)phenyl}ureas
by Kubo, Kazuo and Shimizu, Toshiyuki and Ohyama, Shin-ichi and Murooka, Hideko and Iwai, Akemi and Nakamura, Kazuhide and Hasegawa, Kazumasa and Kobayashi, Yoshiko and Takahashi, Noriko and Takahashi, Kazumi and Kato, Shinichiro and Izawa, Toshio and Isoe, Toshiyuki
Journal of Medicinal Chemistry, ISSN 0022-2623, 03/2005, Volume 48, Issue 5, pp. 1359 - 1366
N-Phenyl-N‘-{4-(4-quinolyloxy)phenyl}ureas were found to be a novel class of potent inhibitors for the vascular endothelial growth factor receptor 2 (VEGFR-2)... 
DESIGN | CHEMISTRY, MEDICINAL | THERAPY | SERIES | ANTI-ANGIOGENESIS | SUPPRESSES | FACTOR RECEPTOR | TUMOR-GROWTH | AUTOPHOSPHORYLATION | CANCER | ENDOTHELIAL GROWTH-FACTOR | Endothelium, Vascular - cytology | Administration, Oral | Humans | Quinolines - chemistry | Angiogenesis Inhibitors - pharmacology | Rats | Structure-Activity Relationship | Quinolines - pharmacology | Quinolines - chemical synthesis | Xenograft Model Antitumor Assays | Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors | Animals | Phenylurea Compounds - chemical synthesis | Mice, Nude | Phenylurea Compounds - chemistry | Cell Proliferation - drug effects | Mice | Phenylurea Compounds - pharmacology | In Vitro Techniques | Umbilical Veins - cytology | Angiogenesis Inhibitors - chemical synthesis | Angiogenesis Inhibitors - chemistry | Endothelial Cells - drug effects
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14. Full Text Biological activities of chitosan and chitooligosaccharides
by Xia, Wenshui and Liu, Ping and Zhang, Jiali and Chen, Jie
Food Hydrocolloids, ISSN 0268-005X, 2011, Volume 25, Issue 2, pp. 170 - 179
Chitosan and its oligosaccharides, which are known to possess multiple functional properties, have attracted considerable interest due to their biological... 
Antimicrobial | Hypocholesterolemic | Biological activities | Chitosan | Chitooligosaccharides | Antitumor | FOOD SCIENCE & TECHNOLOGY | HEXA-N-ACETYLCHITOHEXAOSE | DIFFERENT MOLECULAR-WEIGHTS | BROILER-CHICKENS | RATS | IN-VITRO | ANTIBACTERIAL ACTIVITY | DIFFERENT VISCOSITY | DEACETYLATED CHITOSANS | CHEMISTRY, APPLIED | ANTIMICROBIAL ACTIVITY | CONVERTING-ENZYME | Biomedical materials | Calcium | Iron | Biological | Derivatives | Foods | Oligosaccharides
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