Novel 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues as cytotoxic agents.
A series of 6,7-diphenyl-2,3,8,8a-tetrahydro-1H-indolizin-5-one analogues were synthesized and evaluated for cytotoxic activity against eight human cancer cell lines. Compounds 18, 21, 28, 29, 30 and 31 showed cytotoxic activity with GI(50) values in the range of 2.1-8.1 microM concentration. Among these, compounds 21 and 28 exhibited good pharmacokinetic properties. These compounds were further evaluated for their in vivo efficacy in modified hollow fibre assay (HFA).
Discovery Chemistry, Dr. Reddy's Laboratories, Discovery Research, Miyapur, Hyderabad, 500 050, India. sarmavm@drreddys.com
Vedula M
VM
Sharma
K V
KV
Adi Seshu
C
C
Vamsee Krishna
P
P
Prasanna
V
V
Chandra Sekhar
A
A
Venkateswarlu
Sriram
S
Rajagopal
R
R
Ajaykumar
Dhanvanthri S
DS
Deevi
N V S
NV
Rao Mamidi
R
R
Rajagopalan
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007212:Indolizines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051379:Mice; D010599:Pharmacokinetics; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007212:Indolizines