Abstract
A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.
| Original language | English |
|---|---|
| Pages (from-to) | 2991-2998 |
| Number of pages | 8 |
| Journal | Bulletin of the Korean Chemical Society |
| Volume | 33 |
| Issue number | 9 |
| DOIs | |
| Publication status | Published - 2012 Sep 20 |
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Keywords
- 1,3,4-triarylpyrazole
- A375P
- Anticancer
- Diarylamide
- Diarylurea
ASJC Scopus subject areas
- Chemistry(all)
Cite this
Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold. / Choi, Won Kyoung; El-Gamal, Mohammed I.; Choi, Hong Seok; Hong, Jun Hee; Baek, Daejin; Choi, Kihang; Oh, Chang Hyun.
In: Bulletin of the Korean Chemical Society, Vol. 33, No. 9, 20.09.2012, p. 2991-2998.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Design, synthesis, and preliminary cytotoxicity evaluation of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold
AU - Choi, Won Kyoung
AU - El-Gamal, Mohammed I.
AU - Choi, Hong Seok
AU - Hong, Jun Hee
AU - Baek, Daejin
AU - Choi, Kihang
AU - Oh, Chang Hyun
PY - 2012/9/20
Y1 - 2012/9/20
N2 - A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.
AB - A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3- (trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.
KW - 1,3,4-triarylpyrazole
KW - A375P
KW - Anticancer
KW - Diarylamide
KW - Diarylurea
UR - http://www.scopus.com/inward/record.url?scp=84866406828&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84866406828&partnerID=8YFLogxK
U2 - 10.5012/bkcs.2012.33.9.2991
DO - 10.5012/bkcs.2012.33.9.2991
M3 - Article
VL - 33
SP - 2991
EP - 2998
JO - Bulletin of the Korean Chemical Society
JF - Bulletin of the Korean Chemical Society
SN - 0253-2964
IS - 9
ER -