Recent advances on synthesis and biological activities of C-17 aza-heterocycle derived steroids

H Huo, G Li, B Shi, J Li - Bioorganic & Medicinal Chemistry, 2022 - Elsevier
Steroids modification for improving their biological activities is one of the most efficient and
fruitful methods to develop novel medicines. Steroids with aza-heterocycles attaching to the …

Current advances of tubulin inhibitors in nanoparticle drug delivery and vascular disruption/angiogenesis

S Banerjee, DJ Hwang, W Li, DD Miller - Molecules, 2016 - mdpi.com
Extensive research over the last decade has resulted in a number of highly potent tubulin
polymerization inhibitors acting either as microtubule stabilizing agents (MSAs) or …

Heterocyclic-fused pyrimidines as novel tubulin polymerization inhibitors targeting the colchicine binding site: structural basis and antitumor efficacy

S Banerjee, KE Arnst, Y Wang, G Kumar… - Journal of medicinal …, 2018 - ACS Publications
We report the design, synthesis, and biological evaluation of heterocyclic-fused pyrimidines
as tubulin polymerization inhibitors targeting the colchicine binding site with significantly …

Design, synthesis, and biological evaluation of pyrimidine dihydroquinoxalinone derivatives as tubulin colchicine site-binding agents that displayed potent anticancer …

S Pochampally, KL Hartman, R Wang… - ACS Pharmacology & …, 2023 - ACS Publications
Polymerization of tubulin dimers to form microtubules is one of the key events in cell
proliferation. The inhibition of this event has long been recognized as a potential treatment …

Recent advances in chemistry and pharmacology of 2-methoxyestradiol: An anticancer investigational drug

BS Kumar, DS Raghuvanshi, M Hasanain, S Alam… - Steroids, 2016 - Elsevier
Methoxyestradiol (2ME 2), an estrogen hormone metabolite is a potential cancer
chemotherapeutic agent. Presently, it is an investigational drug under various phases of …

Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin …

YT Wang, YJ Qin, N Yang, YL Zhang, CH Liu… - European journal of …, 2015 - Elsevier
A series of 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives were designed,
synthesized and evaluated as potential tubulin polymerization inhibitors and for the …

Cytotoxicity, in silico predictions and molecular studies for androstane heterocycle compounds revealed potential antitumor agent against lung cancer cells

MA Tantawy, S Shaheen, SW Kattan… - Journal of …, 2022 - Taylor & Francis
Abstract The IL6/JAK2/STAT3 axis dysregulation and the related downstream pathways are
a major contributor to the progression of non-small-cell lung carcinoma (NSCLC) and mainly …

[HTML][HTML] New CDK8 inhibitors as potential anti-leukemic agents–Design, synthesis and biological evaluation

E Solum, TV Hansen, R Aesoy, L Herfindal - Bioorganic & medicinal …, 2020 - Elsevier
Abstract Cyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription
either through its association with the mediator complex or by the phosphorylation of …

Synthesis and Biological Evaluation of 1‐Methyl‐1H‐indole–Pyrazoline Hybrids as Potential Tubulin Polymerization Inhibitors

YL Zhang, YJ Qin, DJ Tang, MR Yang, BY Li… - …, 2016 - Wiley Online Library
Abstract A series of 1‐methyl‐1H‐indole–pyrazoline hybrids were designed, synthesized,
and biologically evaluated as potential tubulin polymerization inhibitors. Among them …

Discovery of novel indole‐1, 2, 4‐triazole derivatives as tubulin polymerization inhibitors

MK Wu, RJ Man, YJ Liao, HL Zhu… - Drug Development …, 2021 - Wiley Online Library
A series of novel indole‐1, 2, 4‐triazole derivatives have been designed, synthesized, and
evaluated as potential tubulin polymerization inhibitors. The top hit 12, bearing the 3, 4, 5 …