Molecules (2019)
Update date:2022-08-22
Topics:
El-Naggar, Mohamed
Sallam, Hanan A.
Shaban, Safaa S.
Abdel-Wahab, Salwa S.
Amr, Abd El-Galil E.
Azab, Mohammad E.
Nossier, Eman S.
Al-Omar, Mohamed A.
A new series of 5-(3,5-dinitrophenyl)-1,3,4-thiadiazole derivatives were prepared and evaluated for their in vitro antimicrobial, antitumor, and DHFR inhibition activity. Compounds 9, 10, 13, and 16 showed strong and broad-spectrum antimicrobial activity comparable to Amoxicillin and Fluconazole as positive antibiotic and antifungal controls, respectively. Compounds 6, 14, and 15 exhibited antitumor activity against four human cancer cell lines, CCRF-CEM leukemia, HCT-15 colon, PC-3 prostate, and UACC-257 melanoma cell lines using Doxorubicin as a reference drug. Compounds 10, 13, 14, and 15 proved to be the most active DHFR inhibitors with an IC50 range of 0.04 ± 0.82–1.00 ± 0.85 μM, in comparison with Methotrexate (IC50 = 0.14 ± 1.38 μM). The highly potent DHFR inhibitors shared a similar molecular docking mode and made a critical hydrogen bond and arene?arene interactions via Ser59 and Phe31 amino acid residues, respectively.
View MoreShanghai Hanshare Industry Co.,Ltd.
Contact:86 21 20960688
Address:RM902-903,Building E, Wanda Plaza,No.26,Zhoukang Road, Pudong District, Shanghai, China
Changzhou Sunlight Pharmaceutical Co., Ltd.
Contact:+86-519-83131668;83139028;83138042;83137041
Address:JiuliStreet, Benniu Town Changzhou City, Jiangsu Province
Liaoyang Xinyou Chemical Products Co.,Ltd.
Contact:+86-419-5165433 13604191870
Address:Huishang Road6-1, Hongwei District, Liaoyang, Liaoning, China
Suzhou SuKaiLu Chemical Technology Co., Ltd.
Contact:+86-512-62766020
Address:Floor 4, Building 1, Xinyi Pharmaceutical Valley Wisdom Industrial Park, 415 Changyang Street, Suzhou Industrial Park, Jiangsu Province
Neworld Chemical Co., Ltd Shanghai
Contact:+86-21-62202658
Address:11F, Blvd 2, No. 1969 PuXing Rd, Shanghai
Doi:10.1134/S107036321512021X
(2015)Doi:10.1021/jo00314a048
(1981)Doi:10.1055/s-0037-1610211
(2018)Doi:10.1002/anie.200462909
(2005)Doi:10.1016/0009-2614(93)89291-O
(1993)Doi:10.1016/S0960-894X(99)00141-9
(1999)