Design, synthesis and biological evaluation of 2,4,5-trisubstituted 7H-Pyrrolo[2,3-d]pyrimidine derivatives as potent EGFR tyrosine kinase inhibitors against the C797S acquired resistance mutation [0.03%]
设计、合成及生物活性评价2,4,5-三取代的7H-吡咯并[2,3-d]嘧啶类化合物作为有效抑制EGFR C797S继发突变的酪氨酸激酶抑制剂
Hao Zhang,Tianlong Lan,Rui Li et al.
Hao Zhang et al.
The C797S mutation in the epidermal growth factor receptor (EGFR) presents a significant challenge in treating non-small cell lung cancer (NSCLC), as it confers resistance to osimertinib. To tackle this issue, we designed and synthesized no...
Discovery of Hsp70 inhibitors for allosteric dissociation of the Hsp70/BAG3 complex via structure-based de novo design [0.03%]
基于结构的从头设计发现Hsp70异位分解Hsp70 / BAG3复合物的抑制剂
Hang Wang,Tong Ji,Jingjing Liu et al.
Hang Wang et al.
Protein-protein interaction (PPI) with cochaperones could induce conformational changes of Hsp70. The Hsp70/BAG3 PPI shows tumor specificity and could be regarded as potential targets for cancer therapy. In this paper, a de novo structure-b...
Synthesis of new 2-styryl-3-nitroimidazo[1,2-a]pyridine derivatives via base-induced elimination of 2-N-tosyl intermediates and in vitro antileishmanial evaluation [0.03%]
通过碱诱导的N-甲苯磺酰基中间体消除合成新的2-茋-3-硝基咪唑并[1,2-a]吡啶衍生物及其体外抗利什曼原虫活性评价
Inès Jacquet,Caroline Castera-Ducros,Romain Paoli-Lombardo et al.
Inès Jacquet et al.
To explore the antileishmanial structure-activity relationships in a 3-nitroimidazo[1,2-a]pyridine series, we developed a previously undescribed olefination strategy at position 2 via elimination of intermediates bearing an N-tosyl group, g...
Design, synthesis, and evaluation of novel tricyclononene carboxamide derivatives as dual anti-orthopoxvirus and anti-inflammatory agents [0.03%]
新型三环壬烯羧酰胺衍生物的设计、合成与评价作为抗正痘病毒和抗炎剂Dual Anti-Orthopoxvirus And Anti-InflammatoryAgents)
Tengxiao Sun,Wei Zheng,Haiguo Sun et al.
Tengxiao Sun et al.
Orthopoxviruses, particularly the monkeypox virus, can cause acute systemic disease accompanied by excessive inflammatory immune responses, while therapeutic options remain limited. In this study, a series of tricyclononene derivatives were...
Synthesis and anti-tumor activity evaluation of novel chalcone derivatives as potential HDAC6 inhibitors [0.03%]
新型查尔康茋衍生物的合成及其作为HDAC6抑制剂的抗肿瘤活性研究
Xin Ma,Siqi Li,Xinyue Huang et al.
Xin Ma et al.
Histone deacetylase inhibitors (HDACis) are a class of epigenetic drugs that, as the name suggests, inhibit histone deacetylases (HDACs), which are anticancer therapeutic targets. Several studies have investigated hydroxamic acid HDACi. How...
Exploration of a novel series of isoindolinone-based hydroxamate derivatives: Design, synthesis, and evaluation of anticancer activity [0.03%]
基于异靛哚啉𬭩类羟胺酸衍生物抗肿瘤活性研究：设计、合成及评价
Xizheng Quan,Yumei Chen,Fangli Ma et al.
Xizheng Quan et al.
Histone deacetylases (HDACs) have been identified as a class of crucial epigenetic enzymes that are responsible for the removal of acetyl groups from the lysine residues in the amino-terminal tails of histones. Their overexpression is close...
Design, synthesis, and biological evaluation of selective cytotoxicity-derived Miliusol derivatives inducing profound TNBC regression in vivo [0.03%]
具有选择性细胞毒性的米利索衍生物的设计、合成及生物学评价诱导活体乳腺癌 regressions
Xiaoling Cheng,Weiji Chen,Wenli Hao et al.
Xiaoling Cheng et al.
Triple-negative breast cancer (TNBC) remains a challenging malignancy due to its aggressive nature and lack of targeted therapies. Miliusol, a natural product isolated from Miliusa tenuistipitata, exhibits potent anti-proliferative activity...
Novel Piperine derivatives containing substituted Benzamide fragments: Design, synthesis, anti-breast cancer activity, and mechanistic study on the PI3K/AKT/mTOR pathway [0.03%]
新型含有取代苯胺片段的胡椒碱衍生物：设计、合成、抗乳腺癌活性及PI3K/AKT/mTOR途径作用机制研究
Mengwei Song,Ying Zhou,Sen Wang et al.
Mengwei Song et al.
Breast cancer is the most prevalent malignant tumor among women worldwide, and recurrence, metastasis, and drug resistance remain major challenges that compromise treatment efficacy and patient prognosis. Piperine has been reported to posse...
3-Deoxy-4-sulfonamido-butein derivatives promote cell cycle arrest and apoptosis by inhibiting EGFR/JAK2/STAT3 signaling in A549 lung cancer cells [0.03%]
3-脱氧-4-磺胺基-白杨茋衍生物通过抑制EGFR/JAK2/STAT3信号通路促进A549肺癌细胞周期阻滞和凋亡
Jung Hwan Choi,Hyun-Ha Hwang,Jinwon Hong et al.
Jung Hwan Choi et al.
Butein, a naturally occurring chalcone, exhibits diverse pharmacological potential but suffers from limited anticancer efficacy. To address this limitation and improve drug-likeness, we designed and synthesized a novel series of 3-deoxy-4-s...
Peptide-drug conjugates bearing an antimitotic Ahx-DA1 payload achieve potent antitumor activity in Her2-amplified and EGFR-positive KRAS-mutant cancers in vivo [0.03%]
含抗微管Ahx-DA1载荷的多肽偶联药物在体内HER2扩增和EGFR阳性KRAS突变癌症中表现出有效的抗肿瘤活性
Akash Panja,Pousali Mitra,Iryna Tkachenko et al.
Akash Panja et al.
Peptide-drug conjugates (PDCs) represent a targeted cancer therapy strategy that combines tumor-homing peptides with potent cytotoxic payloads, offering a promising alternative to antibody-drug conjugates (ADCs) through improved tissue pene...