Abstract
In this article, we detail our latest findings towards developing diversified series of potential non-hormonal contraceptive compounds using a phenotypic screening approach against human sperm. Phenotypic screening of nine compound libraries (88,773 compounds in total) was conducted using an in-house automated robotic screening platform, allowing quantification of sperm motility in samples pre-treated with the compounds. From these screens, 9 chemical series were identified and investigated in hit expansion programs, with a particular focus on identifying chemical matter that selectively reduces sperm motility without any significant cytotoxicity in somatic cells (HepG2 cells). The compounds discussed in this paper could be useful tool compounds for research into non-hormonal contraceptives.
Supplementary materials
Title
Synthetic procedures
Description
Reaction schemes and synthetic procedures of representative compounds from each chemical series
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