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. 2021 Nov 17;13(22):5757. doi: 10.3390/cancers13225757

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© 2021 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

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Structure–activity relationships. (A) PCAIs general structure showing areas of structural variation depicted by “n” and “y”; (B) effect on potency of PCAIs’ tether (linker/N-substituent chain) lengths; (C) effect on potency of the N-cycloalkyl ring size; and (D) comparative effectiveness of S-farnesylated (NSL-YHJ-2-27) versus S-geranylgeranylated (NSL-YHJ-2-89), pyrollidine-capped (NSL-YHJ-2-67) versus methylpiperidine-capped (NSL-YHJ-2-27), and ester-capped (NSL-YHJ-2-84) versus carboxylic acid-capped (NSL-YHJ-3-36) tethers.