Paclitaxel (PTX) is a chemotherapeutic agent which shows antitumor activities against a broad spectrum of cancers. Yet, the current formulation of PTX used in clinic may cause a number of adverse reactions, which significantly limit its application. To obtain better clinical use of PTX, we report, for the first time, iRGD‐PTX conjugate nanoparticles (NPs) for targeted PTX delivery. iRGD‐PTX conjugate was synthesized from thiolated iRGD and 6‐maleimidocaproic acid‐PTX through Michael addition reaction. iRGD‐PTX NPs with hydrodynamic diameter of ~110 nm were self‐assembled from iRGD‐PTX conjugate in deionized water. The as‐prepared iRGD‐PTX NPs exhibit good stability in phosphate buffered saline (PBS) buffer and fetal bovine serum containing PBS buffer. iRGD‐PTX NPs exhibit sustained drug release behaviors. The in vitro studies show that iRGD‐PTX NPs can be internalized by 4T1 cells by integrin αV‐mediated endocytosis, resulting in better in vitro antitumor activity as compared to free PTX. The in vivo studies demonstrate that iRGD‐PTX NPs exhibit enhanced tumor accumulation. The iRGD‐PTX NPs reported here represent a novel PTX nanoplatform to achieve targeted PTX delivery.

A series of substituted acetophenone oxime esters of Pyrithiobac were synthesized as potential herbicides. The structures of the synthesized new compounds were confirmed by 1H NMR, 13C NMR, HRMS, and X‐ray single‐crystal diffraction (XRD). The pre‐emergence and post‐emergence herbicidal activity studies show that 4‐CF3 (6 f), 4‐NO2 (6 i), 4‐NH2 (6 j), 4‐F (6 l), and 2,4‐2OCH3 (6 s) substituted acetophenone oxime esters of Pyrithiobac exhibit better pre‐emergence and post‐emergence herbicidal activities against monocotyledon and dicotyledon weeds than other synthesized new compounds. In pre‐emergence herbicidal activity study, 6 f, 6 i, 6 j, 6 l, and 6 s exhibit similar herbicidal activities against monocotyledon and dicotyledon weeds as compared to Staple (Pyrithiobac‐sodium). In post‐emergence herbicidal activity study, 6 f, 6 i, 6 j, 6 l, and 6 s exhibit similar herbicidal activities against dicotyledon weeds and better herbicidal activities against monocotyledon weeds as compared to Staple. Compounds 6 i and 6 l with high herbicidal activities and similar binding mode with acetolactate synthase as compared to Staple were further subjected to crop safety study. The results show that the safety of compound 6 l to cotton is as good as Staple and better than 6 i. The present work indicates that compound 6 l may serve as a new candidate for potential herbicides.

O‐(2,6‐bis(4,6‐dimethoxypyrimidin‐2‐yloxy)benzoyl)oxime 3‐trifluoromethylacetophenone (HB‐002) was synthesized as potential acetolactate synthetase (ALS)‐inhibiting herbicides. HB‐002 was characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, high resolution mass spectrometer (HRMS), and X‐ray single‐crystal diffraction. The herbicidal activities of HB‐002 against four weeds were studied in greenhouse. The results show that the control effects of HB‐002 on Eclipta prostrata L. and Cyperus difformis are very weak. However, HB‐002 exhibits higher herbicidal activity against Leptochloa chinensis (L.) Nees than that of Pyribenzoxim. HB‐002 also shows certain control effect on Echinochloa oryzoides (Ard.) Flritsch. Molecular docking simulation was performed to study the binding affinity and probable binding modes of HB‐002 with ALS. In the binding mode, the trifluoromethyl group of HB‐002 forms two halogen bonds (fluorine) with ALS, contributing to the lower binding free energy of HB‐002 (‐45.336 kcal/mol) as compared to Pyribenzoxim (‐40.1286 kcal/mol) and m‐trifluoromethyl Pyribenzoxim (‐44.451 kcal/mol). The present work suggests that HB‐002 may serve as a new candidate for potential herbicides.

A series of new trifluoromethyl-substituted phenyl alkyl ketoxime esters of Bispyribac were synthesized as potential herbicides. All synthesized compounds were characterized by nuclear magnetic resonance (NMR) spectroscopy and highresolution mass spectrometry (HRMS). Sprout method and foliar spray method were used to study the herbicidal activity of the synthesized compounds. Among all synthesized compounds, compound 3 (4-trifluoromethylphenyl n-butyl ketoxime ester of Bispyribac) exhibits the highest herbicidal activity against Echinochloa crusgalli (L.) Beauv with median effect dose (ED 50 ) of 1.7 μg/mL in pre-emergence herbicidal activity study. The structure-activity relationship analysis indicates that trifluoromethyl substitution on the phenyl group exhibits better activity than methoxy and methyl substitution on the phenyl group. The alkyl chain length also affects the activity significantly and the optimal alkyl chain length is four among the tested compounds. However, the substitution position of trifluoromethyl exhibits very limited influence on the activity. In post-emergence herbicidal activity study, compound 3 (ED 90 69.1056 g/hm 2 ) exhibits better herbicidal activity against Echinochloa crusgalli (L.) Beauv than Pyribenzoxim (ED 90 99.0810 g/hm 2 ). Moreover, compound 3 exhibits better safety to hybrid rice variety II you 084 and rice variety Nanjing 44 than Pyribenzoxim in crop safety study. Compound 3 may serve as a lead compound for future herbicide discovery.

Three novel 2-phenylthiazole derivatives were synthesised and characterised by spectroscopic techniques. The structure of the synthesised compounds was unambiguously confirmed by a single-crystal X-ray diffraction analysis of ethyl 2-(4-{[5-(4-benzylpiperidin-1-yl)pentyl]oxy}phenyl)thiazole-4-carboxylate. All of the compounds presented good cholinesterase-inhibition activities and ethyl 2-(4-{[5-(4-benzylpiperidin-1-yl)pentyl]oxy}phenyl)thiazole-4-carboxylate showed the best acetylcholinesterase-inhibition and butyrylcholinesterase-inhibition abilities with IC50 values of 5.19 μM and 5.83 μM. The docking study demonstrated that it could interact with both the catalytic active site (CAS) and the peripheral anionic site (PAS) of acetylcholinesterase and could chelate with metal ions like Cu2+ and Zn2+.