Bcr-Abl inhibitors(Bcr-Abl tyrosine kinase inhibitors), SRC inhibitors(Tyrosine-protein kinase SRC inhibitors), p38 MAPK inhibitors(P38 mitogen-activated protein kinase inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication

Chronic Myelogenous Leukemia

Inactive Indication-

Originator Organization-

Active Organization

Chinese Academy of Sciences

Hefei Cosource Pharmaceuticals, Inc.

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC28H26F3N7O2

InChIKeyGXMFPDCIAWSZFR-UHFFFAOYSA-N

CAS Registry1808287-83-3

100 Clinical Results associated with HYMX-053

100 Translational Medicine associated with HYMX-053

100 Patents (Medical) associated with HYMX-053

Literatures (Medical) associated with HYMX-053

28 Nov 2024·Journal of Medicinal Chemistry

Discovery of 5-Nitro-N-(3-(trifluoromethyl)phenyl) Pyridin-2-amine as a Novel Pure Androgen Receptor Antagonist against Antiandrogen Resistance

Article

Author: Zhong, Haiyang ; Sheng, Rong ; Shan, Luhu ; Wang, Huating ; Liao, Jianing ; Cai, Lvtao ; Hou, Tingjun ; Chai, Xin ; Pan, Peichen ; Xu, Lei ; Xu, Xiaohong ; Wang, Xuwen ; Fu, Weitao ; Li, Dan

The transformation of clinical androgen receptor (AR) antagonists into agonists driven by AR mutations poses a significant challenge in treating prostate cancer (PCa). Novel anti-AR therapeutics combating mutation-induced resistance are required. Herein, by combining structure-based virtual screening and biological evaluation, a high-affinity agonist E10 was first discovered. Then guided by the representative conformation of State 1 at the free energy landscape, the structural optimization of E10 was performed, and pure AR antagonists EL15 (IC₅₀ = 0.94 μM) and EF2 (IC₅₀ = 0.30 μM) were successfully identified. Both can antagonize wild-type and variant drug-resistant ARs. Therein, EF2 demonstrated potent inhibition of the AR pathway and effectively suppressed tumor growth in a C4-2B xenograft mouse model following oral administration. Further molecular dynamics simulation and mutagenesis studies revealed atomic insights into the mode of action of EF2 which may serve as a novel lead compound for developing therapeutics against AR-driven PCa.

01 Feb 2022·Acta Crystallographica Section E Crystallographic Communications

Crystal structure and Hirshfeld surface analysis of 5-acetyl-3-amino-6-methyl-N-phenyl-4-[(E)-2-phenylethenyl]thieno[2,3-b]pyridine-2-carboxamide

Article

Author: Mohamed, Shaaban K ; Al-Waleedy, Safiyyah A H ; Mague, Joel T ; Ibrahim, Omaima F ; Bakhite, Etify A ; Çelikesir, Sevim Türktekin ; Akkurt, Mehmet ; Abdu-Allah, Hajjaj H M

The asymmetric unit of the title compound, C25H21N3O2S, comprises four molecules. Their conformations differ primarily in the orientations of the styryl and the N-phenylcarboxamido groups. In the crystal, intermolecular N—H...N, C—H...O and C—H...S hydrogen-bonding contacts as well a C—H...π(ring) interactions lead to the formation of a layer structure parallel to (010). Hirshfeld surface analysis revealed that H...H interactions represent the main contributions to the crystal packing.

28 Oct 2021·Journal of Medicinal ChemistryQ1 · MEDICINE

Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile

Q1 · MEDICINE

Article

Author: Liu, Tao ; Hu, Xiaobei ; Wang, Peipei ; Wang, Chang ; Zhang, Runyuan ; Zhou, Yubo ; Wu, Zhiqi ; Xu, Lei ; Jin, Tingting ; Li, Kun ; Du, Wenxin ; Kan, Weijuan ; Li, Jia

Checkpoint kinase 1 (CHK1) plays an important role in the DNA damage response pathway, being a potential anti-cancer drug target. In this study, we used a strategy for trifluoromethyl substitution to obtain orally bioavailable CHK1 inhibitors to overcome the limitations of lead compound 1, which can only be administered intravenously. After detailed investigation, we identified compound 6c as an oral CHK1 inhibitor, which demonstrated a considerably higher plasma exposure in mice. Compound 6c also showed good kinase selectivity. Moreover, it exhibited a significant antiproliferative effect in MV-4-11 cells singly and a synergistic effect in combination with gemcitabine in HT-29, A549, and RPMI-8226 cells. Additionally, compound 6c could inhibit tumor growth in the MV-4-11 xenograft mouse model. The combination of 6c and gemcitabine exhibited synergistic effect in the HT-29 xenograft mouse model. Thus, compound 6c was found to be a selective and oral potential anticancer CHK1 inhibitor.

100 Deals associated with HYMX-053

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic Myelogenous Leukemia	Preclinical	China	Chinese Academy of Sciences	05 Feb 2016
Chronic Myelogenous Leukemia	Preclinical	China	Hefei Cosource Pharmaceuticals, Inc.	05 Feb 2016

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