Synthesis, biological evaluation and molecular docking of aryl hydrazines and hydrazides for anticancer activity.
Aryl hydrazine and hydrazide analogues were synthesized based on p-tolyl hydrazine, isolated as a breakdown product of a secondary metabolite from the mushroom, Agaricus bisporus, and tested to be highly active molecule than 5-fluorouracil in in vitro anticancer studies. The synthesized analogues were tested for anticancer activity using NCI protocol. Anolgues 12 and 15 emerged as molecules with significant in vitro anticancer activity. Molecular docking study revealed the binding orientations of aryl hydrazines and hydrazides analogues in the active sites of thymidylate synthase.
Department of Natural Products, National Institute of Pharmaceutical Education and Research Sector-67, SAS Nagar, Punjab 160 062, India.
Vikrantsinh M
VM
Gohil
Satyam K
SK
Agrawal
Ajit K
AK
Saxena
Divita
D
Garg
C
C
Gopimohan
Kamlesh K
KK
Bhutani
D000364:Agaricus / Q000737:chemistry; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology*; D001665:Binding Sites; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology*; D006860:Hydrogen Bonding; D008956:Models, Chemical; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D013940:Thymidylate Synthase / Q000737:chemistry / Q000378:metabolism
D000970:Antineoplastic Agents; D006834:Hydrazines; C029424:hydrazine; D013940:Thymidylate Synthase