Hasi, Rumana Yesmin Ali, Hanif Islam, Majidul Habib, Rowshanul Satter, Mohammed A. Yeasmin, Tanzima
Published in
Clinical Phytoscience
BackgroundThe goal of this study was to explore the inherent antioxidant and antineoplastic activities of methanolic extract of the roots of Hibiscus sabdariffa (MEHSR).MethodsThe dried coarse powder of roots of Hibiscus sabdariffa was subjected to methanolic extraction. Here in vitro methods were used to determine the various types of phytochemica...
Soumyanarayanan, Uttara Ramanujulu, Pondy Murugappan Mustafa, Nurulhuda Haider, Shozeb Fang Nee, Adina Huey Tong, Jie Xin Tan, Kevin S W Chng, Wee Joo Dymock, Brian W
Published in
European journal of medicinal chemistry
Herein, we report the discovery of a dual histone deacetylase inhibitor displaying a unique HDAC3/6 selectivity profile. An initial strategy to merge two epigenetic pharmacophores resulted in the discovery of potent HDAC6 inhibitors with selectivity over HDAC1. Screening in an HDAC panel revealed additional low nanomolar inhibition only against HDA...
Abo-Ashour, Mahmoud F Eldehna, Wagdy M Nocentini, Alessio Bonardi, Alessandro Bua, Silvia Ibrahim, Hany S Elaasser, Mahmoud M Kryštof, Vladimír Jorda, Radek Gratteri, Paola
...
Published in
European journal of medicinal chemistry
Herein we describe the design and synthesis of two series of sulfonamides featuring N-unsubstituted (4a-c) or N-substituted (7a-o) isatin moieties (as tails) connected to benzenesulfonamide moiety via a hydrazine linker. All the prepared sulfonamides (4a-c and 7a-o) showed potent inhibitory activities toward transmembrane tumor-associated human (h)...
Lv, Xiao Yang, Xiaoxiao Zhan, Mei-Miao Cao, Peichang Zheng, Shihong Peng, Ruijun Han, Jihong Xie, Zhouling Tu, Zhengchao Liao, Chenzhong
...
Published in
European journal of medicinal chemistry
Polo-like kinase 1 (Plk1) is a validated target for the treatment of cancer. In this report, by analyzing amino acid residue differences among the ATP-binding pockets of Plk1, Plk2 and Plk3, novel selective Plk1 inhibitors were designed based on BI 2536 and BI 6727, two Plk1 inhibitors in clinical studies for cancer treatments. The Plk1 inhibitors ...
Kamarudin, Muhamad Noor Alfarizal Sarker, Md. Moklesur Rahman Zhou, Jin-Rong Parhar, Ishwar
Published in
Journal of Experimental & Clinical Cancer Research
Growing evidence showed the increased prevalence of cancer incidents, particularly colorectal cancer, among type 2 diabetic mellitus patients. Antidiabetic medications such as, insulin, sulfonylureas, dipeptyl peptidase (DPP) 4 inhibitors and glucose-dependent insulinotropic peptide (GLP-1) analogues increased the additional risk of different cance...
Kakkar, Saloni Narasimhan, Balasubramanian
Published in
BMC Chemistry
The utility of oxazole as intermediates for the synthesis of new chemical entities in medicinal chemistry have been increased in the past few years. Oxazole is an important heterocyclic nucleus having a wide spectrum of biological activities which drew the attention of researchers round the globe to synthesize various oxazole derivatives and screen...
Rajoka, Muhammad Shahid Riaz Mehwish, Hafiza Mahreen Hayat, Hafiz Fakhar Hussain, Nazim Sarwar, Sobia Aslam, Humaira Nadeem, Ahmad Shi, Junling
Published in
Probiotics and antimicrobial proteins
The natural antioxidant agent is urgently needed to prevent the negative effects of newly generated free radicals and chronic disorders. Recently, the microbial exopolysaccharide (EPS) is currently used as a potential biopolymer due to its unique biological characteristics. In this study, the biological potential was carried out on the EPSs produce...
Tahlan, Sumit Ramasamy, Kalavathy Lim, Siong Meng Shah, Syed Adnan Ali Mani, Vasudevan Narasimhan, Balasubramanian
Published in
BMC Chemistry
BackgroundDihydrofolate reductase (DHFR) is an important target for antimetabolite class of antimicrobials because it participates in purine synthesis. 2-mercaptobenzimidazole (2MBI) has similar structural features as purine nucleotides. Given that benzimidazole and similar heteroaromatics have been broadly examined for their anticancer potential, ...
Shah, Rashmi Verma, Prabhakar Kumar
Published in
BMC Chemistry
BackgroundA new series of thiophene analogues was synthesized and checked for their in vitro antibacterial, antifungal, antioxidant, anticorrosion and anticancer activities.ResultsA series of ethyl-2-(substituted benzylideneamino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate derivatives were synthesized by using Gewald synthesis and their stru...
Hussein, Essam M. Al-Rooqi, Munirah M. Abd El-Galil, Shimaa M. Ahmed, Saleh A.
Published in
BMC Chemistry
BackgroundSulfonamide derivatives are of great attention due to their wide spectrum of biological activities. Sulfonamides conjugated with acetamide fragments exhibit antimicrobial and anticancer activities. The inhibition dihydrofolate reductase (DHFR) is considered as one of the most prominent mechanism though which sulfonamide derivatives exhibi...
