TY  - JOUR
TI  - Synthesis of some novel hydrazide-hydrazones derived from etodolac as potential anti-prostate cancer agents
AB  - (R,S)-Etodolac [1,8-diethyl-1,3,4,9-tetrahydrapyrano(3,4-b)indole-1-acetic acid] is a nonsteroidal anti-inflammatory drug that contains carboxylic acid group with the structure of pyrano[3,4-b]indole. In this study, a series of novel (R,S)-Etodolac derivatives (3a-l) bearing hydrazide-hydrazone moiety were synthesized. The structures of these compounds were characterized by spectral (1H-NMR and FT-IR analyses) methods. All synthesized compounds were screened for anticancer activity against androgen-independent prostate adenocarcinoma (PC-3, DU-145) and androgen-dependent prostate adenocarcinoma (LNCaP) cell lines by using WST-8 colorimetric method. This method was used for cell viability and cytotoxicity analysis. Compound 3b (SGK-720) [2-(1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(2,6-dichlorophenyl)methylene]hydrazides] showed 10.36, 5.24, 15.53 μM anticancer activity against PC3, DU145, LNCaP cancer cell lines, respectively. According to JC-1 mitochondrial membrane potential test and Annexin V/PI staining, 3b was found to have apoptotic effect on these cancer cells. It is concluded that compound 3b containing 2,6-dichloro substituents may be one of the candidate molecules to cope with prostate cancer.
AU  - Küçükgüzel, Ş.Güniz
AU  - Atlıhan, İrem
AU  - Koç, Hande Cevher
AU  - Orun, Oya
AU  - Mega Tiber, Pinar
DO  - 10.29228/jrp.97
PY  - 2022
JO  - Journal of research in pharmacy (online)
VL  - 26
IS  - 1
SN  - 2630-6344
SP  - 1
EP  - 12
DB  - TRDizin
UR  - http://search/yayin/detay/520427
ER  -