medicinal-chemistry

Mandelate racemase (MR) catalyzes the Mg 2+ -dependent interconversion of ( R )- and ( S )-mandelate and has been employed as a model enzyme to demonstrate that an enzyme catalyzing the deprotonation of a carbon acid substrate may be inhibited by boronic acids. We report a detailed structure–activity-based study of the ability of various boronic acid derivatives to competitively inhibit MR. 2-Nap…

The FDA will allow bemotrizinol in sunscreen. The chemical is long-lasting and defends against solar radiation that ages skin.

Nature Communications, Published online: 12 June 2026; doi:10.1038/s41467-026-74370-9 Direct asymmetric α-C conjugate addition of aminomethylphosphonate to α,β-unsaturated ketones is an intriguing strategy to make bioactive chiral phosphonic 1-pyrrolines. Here, the authors present a direct enantioselective α-C conjugate addition of NH2-unprotected aminomethylphosphonate to α,β-unsaturated ketones…

Nature Communications, Published online: 10 June 2026; doi:10.1038/s41467-026-74372-7 Benzocyclobutenes (BCBs) represent a highly strained, privileged structural motif with significant applications in drug discovery, medicinal chemistry, organic synthesis, polymers and materials science, yet efficient synthetic methods remain limited. Here, the authors report an oxidant-free Au(I)/Au(III)-catalyz…

The Korea Research Institute of Chemical Technology (KRICT, President Seok-Min Shin) announced that its DNA-Encoded Library (DEL) Research Center has launched the "DEL CoreBank Platform," which supports hit discovery processes based on DNA-Encoded Library technology.

BackgroundCeramide, acting as an important second messenger, plays a pivotal role in the induction of apoptosis in cancer cells. As one of the active prenylflavonoid ingredients in Epimedium, icariside I (GH01) has been shown to exhibit significant anticancer activity. However, the mechanism by which GH01 induces tumor cell apoptosis by targeting ceramide-orchestrated signaling remains unclear.Pu…

A Cancer-Fighting Molecule from Tree Bark Has Finally Been Built from Scratch Using a novel approach to obtain a common intermediate, the researchers then employed two bioinspired coupling reactions to complete the total synthesis of bisleuconothine A and bousigonine B for the first time.

In Chinese folk medicine, lily bulbs have traditionally been used to help lower blood glucose levels. Numerous studies have demonstrated that extracts from lily bulbs possess significant hypoglycemic activity. However, the specific active metabolites and their underlying mechanisms remain unclear. This study first evaluated the hypoglycemic activities of extracts from four common lily species: Li…

A package-readiness guide to Pharmaceuticals (MDPI), the medicinal-chemistry and drug-discovery journal distinct from Pharmaceutics: the Susy portal, single-blind review, fast first decision, the 2,900 CHF APC, and the failure patterns that stall medicinal-chemistry manuscripts before review.

Nature Chemistry, Published online: 05 June 2026; doi:10.1038/s41557-026-02164-z A deconstructive alkaloid remodelling strategy comprising a concise set of robust transformations is introduced. Twenty-six altered frameworks are synthesized, requiring an average of ~1.8 steps per analogue. In cellulo evaluation across ten cancer cell lines indicates that an expanded amine bridge and a deconstructe…

A chromosome-level genome has opened a new window into how Hemsleya ellipsoidea, a medicinal cucurbit known as Xuedan, evolved its unusual ability to accumulate cucurbitacin IIa (CuIIa), a bioactive triterpenoid associated with anti-inflammatory and antibacterial activities.

BODIPY-based photosensitizers have attracted great interest in cancer phototherapy and immunotherapy due to their tunable structures, excellent photostability, and high molar extinction coefficients. However, conventional BODIPY dyes have inherent limitations, such as poor water solubility, shallow tissue penetration, oxygen dependence, and insufficient single-modality efficacy. To address these,…

Nature Chemistry, Published online: 01 June 2026; doi:10.1038/s41557-026-02173-y A strategy is developed that merges triplet nitrene-mediated ring expansion with titanium-catalysed cyanylation for the diastereoselective synthesis of vicinal tetrasubstituted cyclobutane amino nitriles. This strategy unlocks highly functionalized and congested three-dimensional cyclobutanes that could provide scaff…

OnLine Journal of Biological Sciences, Published online: 1 June 2026; doi:10.3844/ojbsci.2026.26.02.033 Cyclachaena xanthiifolia is a phytochemically rich invasive weed with documented allelopathic properties, making it a candidate source of bioactive compounds with potential medicinal applications. Thi...