Macrocyclization strategy for improving candidate profiles in medicinal chemistry.
Darlami O, Pun R, Ahn SH, Kim SH, Shin D.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2024.116501 PUBLIKATIONSREGISTRET
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Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2023.115918Neutral sphingomyelinase 2 inhibitors based on the pyrazolo[1,5-a]pyrimidin-3-amine scaffold.
Novotna K, Thomas AG, Stepanek O, Murphy B, Hin N, Skacel J, Mueller L, Tenora L, Pal A, Alt J, Wu Y, Paule J, Rais R, Slusher BS, Tsukamoto T.
Eur J Med Chem · research-article; journal article · DOI 10.1016/j.ejmech.2023.115674Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: A mini review.
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Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.115618Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Xiang S, Wang J, Huang H, Wang Z, Song X, Zhou Y, Jin F, He X, Zhang ZM, Tu Z, Ding K, Zhang Z, Lu X.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114899Design, synthesis and biological evaluation of pyrazolo[3,4-<i>b</i>]pyridine derivatives as TRK inhibitors.
Liu N, Wang X, Fu Q, Qin Q, Wu T, Lv R, Zhao D, Cheng M.
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Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114742Design, synthesis and anti-tumor efficacy of novel phenyl thiazole/triazole derivatives as selective TrkA inhibitors.
Wang X, Tan Z, Wang F, Zhang J, Yang J, Liu S, Jiang N, Zhai X.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2022.116995Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance.
Gong Y, Wu FX, Wang MS, Xu HC, Zhuo LS, Yang GF, Huang W.
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Wang Z, Ren J, Jia K, Zhao Y, Liang L, Cheng Z, Huang F, Zhao X, Cheng J, Song S, Sheng T, Wan W, Shu Q, Wu D, Zhang J, Lu T, Chen Y, Ran T, Lu S.
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Mei LC, Zhuo LS, Xu HC, Huang W, Hao GF, Yang GF.
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Wang Z, Wang J, Wang Y, Xiang S, Song X, Tu Z, Zhou Y, Zhang ZM, Zhang Z, Ding K, Lu X.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.2c00308Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation.
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J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01597Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.
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Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2021.114096Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia.
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Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2021.116596Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation.
Zhuo LS, Wang MS, Wu FX, Xu HC, Gong Y, Yu ZC, Tian YG, Pang C, Hao GF, Huang W, Yang GF.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c01539Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors.
Li P, Cai S, Zhao T, Xu L, Guan D, Li J, Zhou J, Zhang H.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2021.128409Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.
Garrido A, Vera G, Delaye PO, Enguehard-Gueiffier C.
Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113867New Protocol-Guided Exploitation of a Lysosomal Sulfatase Inhibitor to Suppress Cell Growth in Glioblastoma Multiforme.
Zhang MM, Jia Y, Li P, Qiao Y, Qiao Y, Han KL.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.1c00559FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
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Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113218Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.
Zhang Y, Liu Y, Zhou Y, Zhang Q, Han T, Tang C, Fan W.
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Sun M, Cai S, Li P, Zhang F, Zhang H, Zhou J.
Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2020.115811Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Wang B, Zhang W, Liu X, Zou F, Wang J, Liu Q, Wang A, Hu Z, Chen Y, Qi S, Jiang Z, Chen C, Hu C, Wang L, Wang W, Liu Q, Liu J.
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Duan Y, Wang J, Zhu S, Tu ZC, Zhang Z, Chan S, Ding K.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2020.112552Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.
Cui S, Wang Y, Wang Y, Tang X, Ren X, Zhang L, Xu Y, Zhang Z, Zhang ZM, Lu X, Ding K.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.06.064Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application.
Yan W, Lakkaniga NR, Carlomagno F, Santoro M, McDonald NQ, Lv F, Gunaganti N, Frett B, Li HY.
J Med Chem · research-article; journal article; research support, n.i.h., extramural · DOI 10.1021/acs.jmedchem.8b01092