TY - JOUR
T1 - Design, Synthesis and Cytotoxicity Evalufation of Substituted Benzimidazole Conjugated 1,3,4-Oxadiazoles
AU - Quy, Nguyen Phu
AU - Hue, Bui Thi Buu
AU - Do, Kiep Minh
AU - Quy, Ha Thi Kim
AU - De, Tran Quang
AU - Phuong, Tran Thi Bich
AU - Trang, Pham Cong
AU - Quoc, Nguyen Cuong
AU - Morita, Hiroyuki
N1 - Publisher Copyright:
© 2022 The Pharmaceutical Society of Japan
PY - 2022/6/1
Y1 - 2022/6/1
N2 - Two series of 2-substituted benzimidazole conjugated 1,3,4-oxadiazole derivatives were designed, synthesized and evaluated for their cytotoxic activities against the three human cancer cell lines (cervical cancer (HeLa), breast cancer (MCF-7) and lung cancer (A549)). As the results 14 compounds demonstrated consistent to stronger cytotoxicities compared to the control 5-fluorouracil (5-FU) towards the tested cell lines including 4c (HeLa); 4b, 4e, 4h, 7i–j, 7m–n, 7s (MCF-7); 7b (MCF-7, A549); 7h (HeLa, MCF-7); and 4d, 4i, 7c (HeLa, MCF-7, A549), with the IC50 ranging from 2.7 to 38µM. Notably, compound 4b illustrated almost 5-fold activity against the MCF-7 while 4d, 4i were 9- and 8-fold (HeLa), 4.5- and 13-fold (MCF-7), 4.7- and 4-fold (A549) increase in activity compared to 5-FU, respectively, and were found as lead compounds. These findings suggest that compounds 4b, 4d and 4i merit further characterization and can serve as promising scaffolds in the discovery of new potent anticancer agents.
AB - Two series of 2-substituted benzimidazole conjugated 1,3,4-oxadiazole derivatives were designed, synthesized and evaluated for their cytotoxic activities against the three human cancer cell lines (cervical cancer (HeLa), breast cancer (MCF-7) and lung cancer (A549)). As the results 14 compounds demonstrated consistent to stronger cytotoxicities compared to the control 5-fluorouracil (5-FU) towards the tested cell lines including 4c (HeLa); 4b, 4e, 4h, 7i–j, 7m–n, 7s (MCF-7); 7b (MCF-7, A549); 7h (HeLa, MCF-7); and 4d, 4i, 7c (HeLa, MCF-7, A549), with the IC50 ranging from 2.7 to 38µM. Notably, compound 4b illustrated almost 5-fold activity against the MCF-7 while 4d, 4i were 9- and 8-fold (HeLa), 4.5- and 13-fold (MCF-7), 4.7- and 4-fold (A549) increase in activity compared to 5-FU, respectively, and were found as lead compounds. These findings suggest that compounds 4b, 4d and 4i merit further characterization and can serve as promising scaffolds in the discovery of new potent anticancer agents.
KW - Key words benzimidazole
KW - cytotoxicity
KW - heterocycle
KW - hybrid
KW - oxadiazole
UR - http://www.scopus.com/inward/record.url?scp=85131270316&partnerID=8YFLogxK
U2 - 10.1248/cpb.c22-00162
DO - 10.1248/cpb.c22-00162
M3 - 学術論文
C2 - 35650042
AN - SCOPUS:85131270316
SN - 0009-2363
VL - 70
SP - 448
EP - 453
JO - Chemical and Pharmaceutical Bulletin
JF - Chemical and Pharmaceutical Bulletin
IS - 6
ER -