Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures
The vital roles of microtubule in mitosis and cell division make it an attractive target for
antitumor therapy. Colchicine binding site of tubulin is one of the most important pockets that …
antitumor therapy. Colchicine binding site of tubulin is one of the most important pockets that …
Development of combretastatins as potent tubulin polymerization inhibitors
The combretastatins are isolated from South African tree combretum caffrum kuntze. The
lead compound combretastatin A-4 has displayed remarkable cytotoxic effect in a wide …
lead compound combretastatin A-4 has displayed remarkable cytotoxic effect in a wide …
Urea derivatives in modern drug discovery and medicinal chemistry
AK Ghosh, M Brindisi - Journal of medicinal chemistry, 2019 - ACS Publications
The urea functionality is inherent to numerous bioactive compounds, including a variety of
clinically approved therapies. Urea containing compounds are increasingly used in …
clinically approved therapies. Urea containing compounds are increasingly used in …
Styryl group, a friend or foe in medicinal chemistry
D Bhurta, SB Bharate - ChemMedChem, 2022 - Wiley Online Library
Abstract The styryl (Ph‐CH= CH‐R) group is widely represented in medicinally important
compounds, including drugs, clinical candidates, and molecular probes as it positively …
compounds, including drugs, clinical candidates, and molecular probes as it positively …
Design, synthesis, and biological evaluation of novel alkylsulfanyl-1, 2, 4-triazoles as cis-restricted combretastatin A-4 analogues
YH Li, B Zhang, HK Yang, Q Li, PC Diao… - European Journal of …, 2017 - Elsevier
Abstract Thirty-two novel 3-alkylsulfanyl-1, 2, 4-triazole derivatives, designed as cis-
restricted combretastatin A-4 analogues, were synthesized and evaluated for their …
restricted combretastatin A-4 analogues, were synthesized and evaluated for their …
New Potential Agents for Malignant Melanoma Treatment—Most Recent Studies 2020–2022
P Kozyra, D Krasowska, M Pitucha - International Journal of Molecular …, 2022 - mdpi.com
Malignant melanoma (MM) is the most lethal skin cancer. Despite a 4% reduction in mortality
over the past few years, an increasing number of new diagnosed cases appear each year …
over the past few years, an increasing number of new diagnosed cases appear each year …
Combretastatin A-4 analogues with benzoxazolone scaffold: Synthesis, structure and biological activity
MS Gerova, SR Stateva, EM Radonova… - European journal of …, 2016 - Elsevier
In order to design and synthesize a new class of heterocyclic analogues of natural
combretastatin A-4 and its synthetic derivative AVE8062, the benzoxazolone ring was …
combretastatin A-4 and its synthetic derivative AVE8062, the benzoxazolone ring was …
Structure-Activity Relationship Studies of β-Lactam-azide Analogues as Orally Active Antitumor Agents Targeting the Tubulin Colchicine Site
DJ Fu, L Fu, YC Liu, JW Wang, YQ Wang, BK Han… - Scientific Reports, 2017 - nature.com
We have synthesized a series of new β-lactam-azide derivatives as orally active anti-tumor
agents by targeting tubulin colchicine binding site and examined their structure activity …
agents by targeting tubulin colchicine binding site and examined their structure activity …
Synthesis and biological evaluation of N-substituted 3-oxo-1, 2, 3, 4-tetrahydro-quinoxaline-6-carboxylic acid derivatives as tubulin polymerization inhibitors
J Qi, H Dong, J Huang, S Zhang, L Niu, Y Zhang… - European Journal of …, 2018 - Elsevier
A series of novel N-substituted 3-oxo-1, 2, 3, 4-tetrahydro-quinoxaline-6-carboxy-lic acid
derivatives were synthesized and evaluated for their biological activities. Among all …
derivatives were synthesized and evaluated for their biological activities. Among all …
Enhanced anticancer effect of Combretastatin A-4 phosphate when combined with vincristine in the treatment of hepatocellular carcinoma
Tubulin targeting agents have received considerable interest as a potential tumor-selective
vascular disrupting agents, which represent another avenue for cancer growing therapeutic …
vascular disrupting agents, which represent another avenue for cancer growing therapeutic …