[HTML][HTML] Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

A Dhiman, R Sharma, RK Singh - Acta Pharmaceutica Sinica B, 2022 - Elsevier
Cancer, which is the uncontrolled growth of cells, is the second leading cause of death after
heart disease. Targeting drugs, especially to specific genes and proteins involved in growth …

Recent advances in, and challenges of, anti-angiogenesis agents for tumor chemotherapy based on vascular normalization

K Wang, Q Chen, N Liu, J Zhang, X Pan - Drug Discovery Today, 2021 - Elsevier
A major problem associated with cancer treatment is resistance-prone chemotherapeutic
drugs. An increasing number of studies have documented that the occurrence of resistance …

Exploration of novel VEGFR2 tyrosine kinase inhibitors via design and synthesis of new alkylated indolyl-triazole Schiff bases for targeting breast cancer

MS Nafie, ATA Boraei - Bioorganic Chemistry, 2022 - Elsevier
Abstract According to the World Health Organization (WHO) statistics: In 2020, there were
2.3 million women diagnosed with breast cancer and 685,000 deaths globally. Therefore …

Identification of new benzimidazole-triazole hybrids as anticancer agents: multi-target recognition, in vitro and in silico studies

DIA Othman, A Hamdi, SS Tawfik… - Journal of Enzyme …, 2023 - Taylor & Francis
Multi-target inhibitors represent useful anticancer agents with superior therapeutic attributes.
Here in, two novel series of benzimidazole-triazole hybrids were designed, synthesised as …

Synthesis of a new series of pyrazolo [1, 5-a] pyrimidines as CDK2 inhibitors and anti-leukemia

SJ Almehmadi, AMR Alsaedi, MF Harras… - Bioorganic …, 2021 - Elsevier
Based on the structural study of previously known CDK2 inhibitors, a new series of pyrazolo
[1, 5-a] pyrimidine derivatives was designed and synthesized. The target compounds were …

Targeting the interplay between MMP-2, CA II and VEGFR-2 via new sulfonamide-tethered isomeric triazole hybrids; Microwave-assisted synthesis, computational …

MR Aouad, MA Almehmadi, FF Albelwi, M Teleb… - Bioorganic …, 2022 - Elsevier
Recently, the interest in targeting metalloenzymes is obviously growing for halting various
tumor progression events and surmounting the resistance due to routine chemotherapy …

Design and synthesis of new 2-oxoquinoxalinyl-1, 2, 4-triazoles as antitumor VEGFR-2 inhibitors

M Zengin, OU Tan, RK Arafa, A Balkan - Bioorganic Chemistry, 2022 - Elsevier
VEGFR-2 is a tyrosine kinase receptor for VEGFs that play a central role in tumor
angiogenesis. The inhibition of the tyrosine kinase domain of VEGFR-2 has become an …

Biologically Oriented Hybrids of Indole and Hydantoin Derivatives

KA Kochetkov, ON Gorunova, NA Bystrova - Molecules, 2023 - mdpi.com
Indoles and hydantoins are important heterocycles scaffolds which present in numerous
bioactive compounds which possess various biological activities. Moreover, they are …

Novel thiazole derivatives incorporating phenyl sulphonyl moiety as potent BRAFV600E kinase inhibitors targeting melanoma

AY Khormi, TA Farghaly, A Bayazeed, YO Al-Ghamdi… - RSC …, 2022 - pubs.rsc.org
Novel thiazole derivatives possessing phenyl sulfonyl moiety were designed and
synthesized as B-RAFV600E kinase inhibitors based on the clinically-approved anticancer …

Recent Advances and Future Directions on Small Molecule VEGFR Inhibitors in Oncological Conditions

A Thakur, M Rana, A Mishra, C Kaur, CH Pan… - European Journal of …, 2024 - Elsevier
ABSTRACT “A journey of mixed emotions” is a quote that best describes the progress chart
of vascular endothelial growth factor receptor (VEGFR) inhibitors as cancer therapeutics in …