Synthesis, characterization and biological research of novel 2-(quinoline-4-carbonyl)hydrazide-acrylamide hybrids as potential anticancer agents on MCF-7 breast carcinoma cells by targeting EGFR-TK DOI Creative Commons
Hany M. Abd El‐Lateef, Duaa Bafail,

Noura Hamdi Yousef Alhalees

et al.

RSC Advances, Journal Year: 2024, Volume and Issue: 14(32), P. 23495 - 23504

Published: Jan. 1, 2024

A sequence of novel 2-(quinoline-4-carbonyl)hydrazide scaffolds carrying the acrylamide moiety have been synthesized and evaluated for in vitro cytotoxicity against an MCF-7 breast cancer cell line.

Language: Английский

Novel 4-(2-arylidenehydrazineyl)thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico insights DOI

Heba A. Elsebaie,

Eman A. El-Bastawissy,

Kamel M. Elberembally

et al.

Bioorganic Chemistry, Journal Year: 2023, Volume and Issue: 140, P. 106799 - 106799

Published: Aug. 21, 2023

Language: Английский

Citations

23
Poly (ADP-ribose) polymerase (PARP) inhibitors as anticancer agents: An outlook on clinical progress, synthetic strategies, biological activity, and structure-activity relationship DOI
Pronoy Kanti Das, Gurubasavaraja Swamy Purawarga Matada, Rohit Pal

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 274, P. 116535 - 116535

Published: May 31, 2024

Language: Английский

Citations

12
An insight into sustainable and green chemistry approaches for the synthesis of quinoline derivatives as anticancer agents DOI

B. Kumaraswamy,

K. Hemalatha, Rohit Pal

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 275, P. 116561 - 116561

Published: June 7, 2024

Language: Английский

Citations

11
Recent Advances in Structural Optimization of Quinazoline-Based Protein Kinase Inhibitors for Cancer Therapy (2021–Present) DOI Creative Commons
Heba T. Abdel‐Mohsen, Manal M. Anwar, Nesreen S. Ahmed

et al.

Molecules, Journal Year: 2024, Volume and Issue: 29(4), P. 875 - 875

Published: Feb. 16, 2024

Cancer is a complicated, multifaceted disease that can impact any organ in the body. Various chemotherapeutic agents have low selectivity and are very toxic when used alone or combination with others. Resistance one of most important hurdles develop due to use many anticancer therapeutics. As result, treating cancer requires target-specific palliative care strategy. Remarkable scientific discoveries shed light on several molecular mechanisms underlying cancer, resulting development various targeted agents. One heterocyclic motifs quinazoline, which has wide range biological uses chemical reactivities. Newer, more sophisticated medications quinazoline structures been found last few years, great strides made creating effective protocols for building these pharmacologically active scaffolds. A new class known as quinazoline-based derivatives possessing properties consists well-known compounds block different protein kinases other targets. This review highlights recent updates (2021–2024) acting against chemotherapeutics. It also provides guidance design synthesis novel analogues could serve lead compounds.

Language: Английский

Citations

10
Therapeutic potential of anticancer activity of nitrogen-containing heterocyclic scaffolds as Janus kinase (JAK) inhibitor: Biological activity, selectivity, and structure–activity relationship DOI
Rohit Pal, Gurubasavaraja Swamy Purawarga Matada, Ghanshyam Teli

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 152, P. 107696 - 107696

Published: Aug. 8, 2024

Language: Английский

Citations

9
Design, synthesis, and mechanistic insight of novel imidazolones as potential EGFR inhibitors and apoptosis inducers DOI
Fatma G. Abdulrahman, Hamada S. Abulkhair,

Hoda S. El Saeed

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 144, P. 107105 - 107105

Published: Jan. 8, 2024

Language: Английский

Citations

8
Design, synthesis, and biological evaluation of novel 4-(4-ethoxyphenyl)-6-(substituted-phenyl)pyrimidin-2-amine/thiol/hydroxy derivatives as EGFRWT and EGFRT790M inhibitors targeting NSCLC: In-vitro and in-silico exploration DOI
Rohit Pal, Gurubasavaraja Swamy Purawarga Matada, Ghanshyam Teli

et al.

Journal of Molecular Structure, Journal Year: 2025, Volume and Issue: 1327, P. 141227 - 141227

Published: Jan. 2, 2025

Language: Английский

Citations

1
Synthetic product-based approach toward potential antileishmanial drug development DOI
Rohit Pal, Ghanshyam Teli, Md Jawaid Akhtar

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 263, P. 115927 - 115927

Published: Nov. 11, 2023

Language: Английский

Citations

18
Nitrogen‐Containing Heterocyclic Scaffolds as EGFR Inhibitors: Design Approaches, Molecular Docking, and Structure‐Activity Relationships DOI
Rohit Pal, Ghanshyam Teli, Gurubasavaraja Swamy Purawarga Matada

et al.

ChemistrySelect, Journal Year: 2023, Volume and Issue: 8(26)

Published: July 10, 2023

Abstract Cancer is a wide collection of diseases and among the numerous pathways involved in cancer pathogenesis, pathway involving epidermal growth factor receptor (EGFR) one most prominent. EGFR frequently articulated variety such as breast cancer, pancreatic non‐small cell lung (NSCLC), head neck cancer. There are different tyrosine kinase inhibitors (TKIs) approved by FDA for treatment However, none them evidenced boon to oncological medical department. Frequently occurrence inherent acquired resistance TKIs result mutations principal cause current situation. Therefore, researchers desire evolving novel TKIs. Further, N ‐heterocyclic ring system always proved be magical weapon designed discovery synthetic molecules they comprehensive range pharmacological properties. In recent year (2018–2022) derivatives were uncovered potential The present review summarised research progress dazed limitations currently accessible drugs consecrating, anatomy, mutation EGFR, its role types highlights medicinal chemistry prospective emphasising about designing strategies, docking studies, biological evaluation, selectivity structural activity relationship compounds. Our will support chemists direction development based

Language: Английский

Citations

17
Pyrazole, Pyrazoline, and Fused Pyrazole Derivatives: New Horizons in EGFR‐Targeted Anticancer Agents DOI
Ketan R Hosamani, K. Hemalatha, Rohit Pal

et al.

Chemistry & Biodiversity, Journal Year: 2024, Volume and Issue: 21(11)

Published: July 26, 2024

Pyrazole and its derivatives remain popular heterocycles in drug research, design, development. Several drugs include the pyrazole scaffold, such as ramifenazone, ibipinabant, antipyrine, axitinib, etc. They have been extensively studied by scientific community are said to a wide range of biological activity, especially anticancer agents targeting EGFR. Overexpression EGFR signalling promotes tumor growth inhibiting apoptosis. dysfunction has described multiple cancers, including colon, head neck, NSCLC, liver, breast, ovarian cancer. As result, represents prospective target for cancer treatment. anti-EGFR thriving, notably dacomitinib, afatinib, erlotinib, gefitinib, osimertinib. However, almost all currently available limited therapeutic effectiveness due lack selectivity well substantial side effects. Furthermore, aberrant across numerous human malignancies/carcinomas is impeded gene amplification, protein overexpression, mutations, or in-frame deletions, making EGFR-induced treatment challenging. To overcome such, novel with high efficacy minimal toxicity required. battle resistance inhibitors, pyrazole, pyrazoline, their investigated viable pharmacophore development new better potency, lesser toxicity, favourable pharmacokinetic characteristics. The present investigation covers examination progress toward anti-cancer therapies via fused pyrazole-based compounds. current study also inclusive data on marketed candidates undergoing preclinical clinical Lastly, we discussed recent advances medicinal chemistry significance eradication various cancers provide direction structure-activity relationship (SAR), mechanistic studies.

Language: Английский

Citations

5