The recent progress of isoxazole in medicinal chemistry

J Zhu, J Mo, H Lin, Y Chen, H Sun - Bioorganic & Medicinal Chemistry, 2018 - Elsevier
Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities.
Developing compounds with heterocycle rings has been one of the trends. The integration of …

The molecular basis for RET tyrosine-kinase inhibitors in thyroid cancer

V De Falco, F Carlomagno, H Li, M Santoro - Best practice & research …, 2017 - Elsevier
RET receptor tyrosine kinase acts as a mutated oncogenic driver in several human
malignancies and it is over-expressed in other cancers. Small molecule compounds with …

Pyrrolo[2′,3′:3,4]cyclohepta[1,2-d][1,2]oxazoles, a New Class of Antimitotic Agents Active against Multiple Malignant Cell Types

V Spano, R Rocca, M Barreca… - Journal of medicinal …, 2020 - ACS Publications
A new class of pyrrolo [2′, 3′: 3, 4] cyclohepta [1, 2-d][1, 2] oxazoles was synthesized for
the treatment of hyperproliferative pathologies, including neoplasms. The new compounds …

Generation of an 4‐Isoxazolyl Anion Species: Facile Access to Multifunctionalized Isoxazoles

T Morita, S Fuse, H Nakamura - … Chemie International Edition, 2016 - Wiley Online Library
A direct functionalization of unsubstituted isoxazole (1) was achieved by generation of 4‐
isoxazolyl anion species (3). An efficient 4‐iodination of isoxazole and halogen–metal …

1-Methyl-3-((4-(quinolin-4-yloxy) phenyl) amino)-1H-pyrazole-4-carboxamide derivatives as new rearranged during transfection (RET) kinase inhibitors capable of …

Y Zhang, S Chan, R He, Y Liu, X Song, ZC Tu… - European Journal of …, 2022 - Elsevier
REarranged during Transfection (RET) is a validated target for anticancer drug discovery
and two selective RET inhibitors were approved by US FDA in 2020. However, acquired …

Synthesis and structure–activity relationship study of pyrazolo [3, 4-d] pyrimidines as tyrosine kinase RET inhibitors

C Wang, H Liu, Z Song, Y Ji, L Xing, X Peng… - Bioorganic & medicinal …, 2017 - Elsevier
Abstract Three series of pyrazolo [3, 4-d] pyrimidine derivatives were synthesized and
evaluated as RET kinase inhibitors. Compounds 23a and 23c were identified to show …

First SAR study for overriding NRAS mutant driven acute myeloid leukemia

H Cho, I Shin, E Ju, S Choi, W Hur, H Kim… - Journal of Medicinal …, 2018 - ACS Publications
GNF-7, a multitargeted kinase inhibitor, served as a dual kinase inhibitor of ACK1 and GCK,
which provided a novel therapeutic strategy for overriding AML expressing NRAS mutation …

Design and Synthesis of Novel Thieno[3,2-c]quinoline Compounds with Antiproliferative Activity on RET-Dependent Medullary Thyroid Cancer Cells

G La Monica, G Pizzolanti, C Baiamonte, A Bono… - ACS …, 2023 - ACS Publications
RET kinase gain-of-function mutations represent the main cause of the high aggressiveness
and invasiveness of medullary thyroid cancer (MTC). The selective inhibition of the RET …

[1, 2] Oxazolo [5, 4-e] isoindoles as promising tubulin polymerization inhibitors

V Spanò, M Pennati, B Parrino, A Carbone… - European Journal of …, 2016 - Elsevier
Abstract A series of [1, 2] Oxazolo [5, 4-e] isoindoles has been synthesized through a
versatile and high yielding sequence. All the new structures showed in the 1 HNMR spectra …

Discovery of 4-methyl-N-(4-((4-methylpiperazin-1-yl) methyl)-3-(trifluoromethyl) phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo [3, 4-d] pyrimidin-4-yl)-oxy) benzamide as a …

X Li, J Su, Y Yang, W Lian, Z Deng, Z Yang… - European Journal of …, 2020 - Elsevier
The receptor tyrosine kinase rearranged during transfection (RET) plays pivotal roles in
several cancers, including thyroid carcinoma and non-small cell lung cancer (NSCLC) …