Design and Structural Optimization of Orally Bioavailable SOS1 Inhibitors for the Treatment of KRAS-Driven Carcinoma.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01517
Abstract: KRAS mutations (G12C, G12D, etc.) are implicated in the oncogenesis and progression of many refractory cancers. Son of sevenless homolog 1 (SOS1) is a key regulator of KRAS to modulate KRAS from inactive to active… read more here.
Keywords: optimization orally; design structural; structural optimization; kras driven ... See more keywords
Optimization of Orally Bioavailable Antileishmanial 2,4,5-Trisubstituted Benzamides.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00056
Abstract: Leishmaniasis, a neglected tropical disease caused by Leishmania species parasites, annually affects over 1 million individuals worldwide. Treatment options for leishmaniasis are limited due to high cost, severe adverse effects, poor efficacy, difficulty of use,… read more here.
Keywords: chemistry; orally bioavailable; trisubstituted benzamides; antileishmanial trisubstituted ... See more keywords
Optimization of Orally Bioavailable PI3Kδ Inhibitors and Identification of Vps34 as a key off-target activity.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01585
Abstract: Optimisation of a lead series of PI3Kδ inhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for the class III… read more here.
Keywords: orally bioavailable; pi3k; optimization orally; compound ... See more keywords