Phytochemical analysis and bioactivity screening of three medicinal plants of Saudi Arabia

Purpose: To investigate the phytochemical analysis and bioactivity screening of some Asteraceae medicinal plants. Methods: The chemical constituents were isolated by column chromatography and elucidated using chemical and extensive spectroscopic methodologies including gas chromatoraphy-mass spectrometry (GC-MS), Fourier transform infrared spectroscopy (FTIR), as well as 1D and 2D nuclear magnetic resonance (NMR). The plant extracts were obtained by solvent extraction method while hydrodistillation was used to isolate plant essential oils. Furthermore, cup-plate agar diffusion was applied for antimicrobial activity evaluation while minimum inhibitory concentration (MIC) was assessed by microdilution technique. Results: Centaurea pseudosinaica, Tripleurospermum auriculatum, and Koelpinia linearis afforded previously undescribed three coumarins (xanthotoxin, cirsimaritin, salvigenins) from C. pseudosinaica, one steroid (estradiol) and a pentacyclic triterpene (β-amyrin) from T. auriculatum and a coumarin (santin) from K. linearis in good yields. In addition, the plant extracts and oils exhibited remarkable bioactivities including antifungal, antibacterial and antipyretic etc. Conclusion: The results reveal the presence of bioactive phytomolecules from Asteraceae plant extracts and volatile oils from three Asteraceae plants. Keywords: C. pseudosinaica, T. auriculatum, K. linearis, Xanthotoxin, Salvigenin, Cirsimaritin, Santin, Estradiol, β-amyrin, Antimicrobial activit

Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4-b]indol-3-one Derivatives as Potent Inhibitors of EGFRT790M/BRAFV600E Pathways

Funding Information: This work was funded by Princess Nourah bint Abdulrahman University Researchers Supporting Project Number (PNURSP2023R3), Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.Peer reviewedPublisher PD

Crystal structure of 2-(adamantan-1-yl)-5-(3,5-dinitrophenyl)-1,3,4-oxadiazole, C18H18N4O5

C18H18N4O5, monoclinic, P21/c (no. 14), a = 11.7553(8) Å, b = 6.4876(4) Å, c = 22.3442(15) Å, β = 91.263(7)°, V = 1703.64(19) Å3, Z = 4, Rgt (F) = 0.0531, wRref (F 2) = 0.1376, T = 160 K. CCDC no.: 2173380 The molecular structure is shown in the figure. Table 1 contains crystallographic data and Table 2 contains the list of the atoms including atomic coordinates and displacement parameters

Crystal structure of 4-ethyl-2-{[(4-nitrophenyl)methyl]sulfanyl}-6-oxo-1,6-dihydropyrimidine-5-carbonitrile, C14H12N4O3S

C14H12N4O3S, monoclinic, P21/n (no. 14), a = 12.2777(3) Å, b = 9.4312(2) Å, c = 12.9412(2) Å, β = 107.945(2)°, V = 1425.61(5) Å3, Z = 4, R gt (F) = 0.0305, wR ref (F 2) = 0.0837, T = 160 K. CCDC no.: 2059188 The molecular structure is shown in the figure. Table 1 contains crystallographic data and Table 2 contains the list of the atoms including atomic coordinates and displacement parameters

Crystal structure of 4-chloro-<i>N</i>′-[(1<i>E</i>)-pyridin-3-ylmethylidene]benzohydrazide, C₁₃H₁₀ClN₃O

C13H10ClN3O, monoclinic, P21/c (no. 14), a = 19.0933(2) Å, b = 23.0910(3) Å, c = 10.6831(2) Å, β = 90.064(1)°, V = 4710.00(12) Å3, Z = 16, R gt (F) = 0.0411, wR ref (F 2) = 0.1081, T = 160 K. CCDC no.: 223377

Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides as Potential Multi-Target Antiproliferative Agents

Funding Information: The author acknowledge the support by Princess Nourah Bint Abdulrahman University Researchers Supporting Project Number (PNURSP2023R3), Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.Peer reviewedPublisher PD

Crystal structure of N-ethyl-4-[3-(trifluoromethyl)-phenyl]piperazine-1-carbothioamide, C14H18F3N3S

C14H18F3N3S, monoclinic, P2(1)/c (no. 14), a = 4.61919(4) angstrom, b = 29.1507(3) angstrom, c = 11.27803(10) angstrom, beta = 94.4768(8)degrees, V = 1513.99(3) angstrom(3), Z = 4, R- gt (F) = 0.0588, wR( ref )(F-2) = 0.1579, T = 160 K

Crystal structure of 2-({[5-(adamantan-2-yl)-2-sulfanylidene-1,3,4-oxadiazolidin-3-yl]methyl}amino)benzonitrile, C20H22N4OS

C20H22N4OS, triclinic, P (1) over bar (no. 2), a = 6.8528(3) angstrom, b = 11.3498(5) angstrom, c = 13.3896(9) angstrom, alpha = 114.083(5)degrees, beta = 104.326(4)degrees, gamma = 90.369(3)degrees, V = 914.38(9) angstrom(3), Z = 2, R-gt(F) = 0.0844, wR(ref)(F-2) = 0.2217, T = 160 K

Crystal structure of 4-chloro-<i>N</i>′-[(1<i>E</i>)-(2-nitrophenyl)methylidene]benzohydrazide, C₁₄H₁₀ClN₃O₃

C14H10ClN3O3, triclinic, P1 (no. 1), alpha = 4.8813(2) angstrom, b = 6.7806(2) angstrom, c = 10.3135(2) angstrom, alpha = 98.101( 2)degrees, ss = 94.174( 2)degrees,gamma= 97.612( 3)degrees, V = 333.515(18) angstrom(3), Z = 1, R-gt(F) = 0.0270, wR(ref) (F-2 )= 0.0743, T = 160 K

Synthesis and Biological Evaluation of Indole-2-Carboxamides with Potent Apoptotic Antiproliferative Activity as EGFR/CDK2 Dual Inhibitors

Funding Information: This work was funded by Princess Nourah bint Abdulrahman University Researchers Supporting Project Number (PNURSP2022R3), Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.Peer reviewedPublisher PD