A decade of tail-approach based design of selective as well as potent tumor associated carbonic anhydrase inhibitors
Human carbonic anhydrase (hCA) isoforms hCA IX and hCA XII are well established
anticancer drug targets and their selective inhibition is highly desired for the proper …
anticancer drug targets and their selective inhibition is highly desired for the proper …
Fluorine in anti-HIV drugs approved by FDA from 1981 to 2023
S Han, Y Lu - European Journal of Medicinal Chemistry, 2023 - Elsevier
Human immunodeficiency virus (HIV) is the etiological agent of acquired immunodeficiency
syndrome (AIDS). Nowadays, FDA has approved over thirty antiretroviral drugs grouped in …
syndrome (AIDS). Nowadays, FDA has approved over thirty antiretroviral drugs grouped in …
Ligand-based design on the dog-bone-shaped BIBR1532 pharmacophoric features and synthesis of novel analogues as promising telomerase inhibitors with in vitro …
Telomerase is an outstanding biological target for cancer treatment. BIBR1532 is a non-
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
nucleoside selective telomerase inhibitor; however, it experiences ineligible …
Lead optimization of BIBR1591 to improve its telomerase inhibitory activity: design and synthesis of novel four chemical series with in silico, in vitro, and in vivo …
AA Al-Karmalawy, MHA Mousa… - Journal of Medicinal …, 2023 - ACS Publications
Herein, modifications to the previously reported BIBR1591 were conducted to obtain
bioisosteric candidates with improved activities. The% inhibition of the newly afforded …
bioisosteric candidates with improved activities. The% inhibition of the newly afforded …
Click chemistry approaches for developing carbonic anhydrase inhibitors and their applications
A Angeli, CT Supuran - Journal of Enzyme Inhibition and Medicinal …, 2023 - Taylor & Francis
Click chemistry reactions constitute an important and relatively new approach in the
medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms …
medicinal chemistry toolbox and offer substantial advantages to medicinal chemists in terms …
Carbonic anhydrase inhibitors: an update on experimental agents for the treatment and imaging of hypoxic tumors
CT Supuran - Expert Opinion on Investigational Drugs, 2021 - Taylor & Francis
Introduction Hypoxic tumors, unlike normal tissues, overexpress proteins involved in oxygen
sensing, metabolism, pH regulation, angiogenesis, immunological response, and other …
sensing, metabolism, pH regulation, angiogenesis, immunological response, and other …
Effect of an Imidazole-Containing Schiff Base of an Aromatic Sulfonamide on the Cytotoxic Efficacy of N,N-Coordinated Half-Sandwich Ruthenium(II) p-Cymene …
M Maji, S Acharya, I Bhattacharya, A Gupta… - Inorganic …, 2021 - ACS Publications
Sulfonamides have a broad range of therapeutic applications, which include the inhibition of
various isoforms of carbonic anhydrases (CAs). Among the various CA isoforms, CA IX is …
various isoforms of carbonic anhydrases (CAs). Among the various CA isoforms, CA IX is …
Chalcogenides-incorporating carbonic anhydrase inhibitors concomitantly reverted oxaliplatin-induced neuropathy and enhanced antiproliferative action
Platinum-based chemotherapy is widely used for the treatment of different tumors but is
associated with serious side effects, among which neuropathic pain. Carbonic anhydrase …
associated with serious side effects, among which neuropathic pain. Carbonic anhydrase …
Novel insights on human carbonic anhydrase inhibitors based on coumalic acid: design, synthesis, molecular modeling investigation, and biological studies
V Pontecorvi, M Mori, F Picarazzi, S Zara… - International Journal of …, 2022 - mdpi.com
Human carbonic anhydrase (hCA, EC 4.2. 1.1) isoforms IX and XII are overexpressed in
solid hypoxic tumors, and they are considered as prognostic tools and therapeutic targets for …
solid hypoxic tumors, and they are considered as prognostic tools and therapeutic targets for …
New genetic bomb trigger: Design, synthesis, molecular dynamics simulation, and biological evaluation of novel BIBR1532-related analogs targeting telomerase …
Telomeres serve a critical function in cell replication and proliferation at every stage of the
cell cycle. Telomerase is a ribonucleoprotein, responsible for maintaining the telomere …
cell cycle. Telomerase is a ribonucleoprotein, responsible for maintaining the telomere …