Computational chemistry in drug lead discovery and design

CN Cavasotto, MG Aucar… - International Journal of …, 2019 - Wiley Online Library
The main contributions of our group during the last 15 years developing and using
biomolecular simulation tools in drug lead discovery and design, in close collaboration with …

Design, synthesis, X-ray crystal structures, anticancer, DNA binding, and molecular modelling studies of pyrazole–pyrazoline hybrid derivatives

M Rana, H Hungyo, P Parashar, S Ahmad… - RSC …, 2023 - pubs.rsc.org
We have designed and synthesized three pyrazole analogs (4, 5a, 5b), pyrazole-based
chalcones (6a–6d) and (8a–8h), and N-formyl/acetyl 1, 3, 5-trisubstituted pyrazoline analogs …

Cooperative triple catalysis enables regioirregular formal Mizoroki–Heck reactions

K Liu, D Leifert, A Studer - Nature Synthesis, 2022 - nature.com
Abstract The Mizoroki–Heck reaction between alkenes and aryl halides represents one of
the most important methods for C− C bond formation in synthetic chemistry. Governed by …

Overcoming paradoxical kinase priming by a novel MNK1 inhibitor

E Bou-Petit, S Hümmer, H Alarcon… - Journal of Medicinal …, 2022 - ACS Publications
Targeting the kinases MNK1 and MNK2 has emerged as a valuable strategy in oncology.
However, most of the advanced inhibitors are acting in an adenosine triphosphate (ATP) …

Design, synthesis and evaluation of azaacridine derivatives as dual-target EGFR and Src kinase inhibitors for antitumor treatment

Z Cui, S Chen, Y Wang, C Gao, Y Chen, C Tan… - European Journal of …, 2017 - Elsevier
Overexpression of EGFR is often associated with advanced stage disease and poor
prognosis. In certain cancers, Src works synergistically with EGFR to promote proliferation …

Novel dihydrobenzofuran derivatives: design, synthesis, cytotoxic activity, apoptosis, molecular modelling and DNA binding studies

M Rana, I Ansari, C Twala, S Khan… - Journal of …, 2023 - Taylor & Francis
Abstract Pyrazoline derivatives (3a–3e) and (4a–4e) were designed and synthesized
through chalcones (2a–2e) cyclization with NH2NH2/HCOOH and NH2CSNHNH2 …

Ligand binding effects on the activation of the EGFR extracellular domain

Q Shao, W Zhu - Physical Chemistry Chemical Physics, 2019 - pubs.rsc.org
The epidermal growth factor receptor (EGFR) is one of the most common target proteins in
anti-cancer therapy. The binding of the EGF ligand to the EGFR extracellular domain (EGFR …

Synthesis of new 4-amino-substituted 7-iminopyrido[2,3-d]pyrimidines

AN Zinchenko, LV Muzychka, II Biletskii… - Chemistry of Heterocyclic …, 2017 - Springer
The reaction of 4, 6-dichloropyrimidine-5-carbaldehyde with
cyanomethyltriphenylphosphonium chloride gave (2 Е)-3-(4, 6-dichloropyrimidin-5-yl) …

One‐Pot Synthesis of 6‐Aminopyrido[2,3‐d]pyrimidin‐7‐ones

AM Zinchenko, LV Muzychka… - European Journal of …, 2018 - Wiley Online Library
One‐pot synthesis of 6‐aminopyrido [2, 3‐d] pyrimidin‐7‐ones from 4‐aminopyrimidine‐5‐
carbaldehydes and the in situ N‐protected methyl glycinate is developed. The obtained …

[HTML][HTML] Synthesis and biological evaluation of novel amino-substituted derivatives of pyrido [2, 3-d] pyrimidine as inhibitors of protein kinase CK2

AN Zinchenko, LV Muzychka, OB Smolii… - Biopolymers and …, 2017 - biopolymers.org.ua
Aim. A search for human protein kinase CK2 inhibitors in a series of new amino-substituted
pyrido [2, 3-d] pyrimidine derivatives. Methods. Organic synthesis, analytical and spectral …