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The medicinal plant Haloxylon salicornicum is utilized for therapeutic purposes. We previously reported the antioxidant potential of hexane fraction and methanol extracts of the same species. However, since these solvents could be clinically toxic, the current findings investigated the pharmacological effects of the water fraction. The pain relieving, antioxidant, anti-inflammatory, and antipyretic potential of H. salicornicum water extract (HEW) were studied at two concentrations (250 and 500 mg/kg) in rodents. The carrageenan stimulated rat paw edema assay was exercised to assess anti inflammatory potential in rats; yeast-stimulated hyperthermia was utilized to test antipyretic activity in mice; analgesic properties were assessed based on acetic acid-induced writhing, tail flicking, and hot-plate test; and antioxidant potential was examined with the 2,2-diphenyl-1-picrylhydrazyl assay. We found that 500 mg/kg HEW inhibited edema by 44.03%. Yeast-induced hyperthermia in mice was reduced by 250 and 500 mg/kg HEW after 30, 60, and 120 min with significant level of (P < 0.001) compared to rectal temperature of yeast administered group. The high dose of HEW (500 mg/kg) improved the reaction time of mice in the hot-plate test from 6.66 ± 0.33 to 11.33 ± 0.49 s after 120 min. In the acetic acid-stimulated writhing test, 250 and 500 mg/kg HEW decreased writhing by 32.71% and 51.40%, respectively, after 20 min. HEW also showed antioxidant effects. These results demonstrate that HEW is bioactive and has therapeutic potential for treating a variety of ailments.

The detoxification, metabolism, and excretion of various endogenous and exogenous materials occur mainly in the liver. Liver diseases are a global concern, and classified as chronic hepatitis, cirrhosis, and hepatosis. The development of safe hepatoprotective agents remains an unmet need. Therefore, we investigated the antioxidant effects of methanolic and n-hexane fractions of Zilla spinosa (ZSM and ZSH, respectively) and Hammada elegans (HEM and HEH, respectively) against carbon tetrachloride (CCl4)-induced liver toxicity in rats. Antioxidant activity was studied by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The rats were divided into 11 groups (n=6)–group, 1 (control), group 2 (CCl4 only), group 3 (CCl4+silymarin 10 mg/kg), group 4 (CCl4+HEM 250 mg/kg), group 5 (CC14+HEM 500 mg/kg), group 6 (CCl4+HEH 250 mg/kg), group, 7 (CCl4+HEH 500 mg/kg), group, 8 (CCl4+ZSM 250 mg/kg), group 9 (CCl4+ZSM 500 mg/kg), group 10 (CCl4+ZSH 250 mg/kg), and group 11 (CCl4+ZSH 500 mg/kg). Serum levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, gamma glutamyl transferase, and total bilirubin were measured. The extent of hepatic injury was histopathologically assessed. Treatment with ZSM and ZSH at 250 and 500 mg/kg did not significantly affect biochemical results compared with the CCl4 only group. However, treatment with both HEM and HEH at 250 and 500 mg/kg provided significant (p

As a part of ongoing studies in developing new anticancer agents, novel 1,2-dihydropyridine 4, thienopyridine 5, isoquinolines 6–20, acrylamide 21, thiazolidine 22, thiazoles 23–29 and thiophenes 33–35 bearing a biologically active quinoline nucleus were synthesized. The structure of newly synthesized compounds was confirmed on the basis of elemental analyses and spectral data. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. 2,3-Dihydrothiazole-5-carboxamides 27, 25, 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (34), 1,2-dihydroisoquinoline-7-carbonitrile (7), 5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide (35), 1,2-dihydroisoquinoline-7-carbonitrile (6), 2-cyano-3-(dimethylamino)-N-(quinolin-3-yl)acrylamide (21), 1,2-dihydroisoquinoline-7-carbonitriles (11) and (8) exhibited higher activity (IC50 values of 27–45 μmol L–1) compared to doxorubicin (IC50 47.9 μmol L–1). LQ quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (12), 2-thioxo-2,3-dihydrothiazole-5-carboxamide (28) and quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (15) show activity comparable to doxorubicin, while (quinolin-3-yl)-1,2-dihydroisoquinoline-7-carbonitrile (9), 2,3-dihydrothiazole-5-carboxamide (24), thieno [3,4-c] pyridine-4(5H)-one (5), cyclopenta[b]thiophene-3-carboxamide (33) and (quinolin-3-yl)-6-stryl-1,2-dihydroisoquinoline-7-carbonitrile (10) exhibited moderate activity, lower than doxorubicin.

C23H28N4O6S, triclinic, P1̅ (no. 2), a = 7.3612(3) Å, b = 9.2370(4) Å, c = 19.2940(8) Å, α = 94.657(2)°, β = 96.902(2)°, γ = 113.010(2)°, V = 1186.92(9) Å3, Z = 2, Rgt(F) = 0.0617, wRref(F2) = 0.1575, T = 100 K.

To discover new bioactive lead compounds for medicinal purposes, 2-cyano-3-(4-substituted)-N-(quinolin-3-yl) acrylamide derivatives 2–24, chromenes 25, 26 and benzochromenes 27, 28 were synthesized. The structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectroscopies. In addition, the structure of compound 1 was confirmed through X-ray crystallography. All the newly synthesized compounds were evaluated for their cytotoxic activity against the breast cancer cell line MCF7. The corresponding 2-cyano-3-(4-hydroxy-3-methoxyphenyl)-N-(quinolin-3-yl) acrylamide (15), 3-oxo-N-(quinolin-3-yl)-3H-benzol[f] chromene-2-carboxamide (27), 2-cyano-3-(4-fluorophenyl-N-(quinolin-3-yl) acrylamide (7), 2-cyano-5-(4-(dimethyl-amino) phenyl)-N-(quinolin-3-yl) penta-2,4-dienamide (19) exhibited higher activity compared to doxorubicin (with IC50 value of 47.9 μmol L−1) as a reference drug, with IC50 values of 29.8, 39.0, 40.0, 40.4 μmol L−1, resp. Also, quinoline acrylamides containing 2,3,4-trimethoxyphenyl 17, 2-chlorophenyl 10, benzo[d][1,3]dioxol 12, 2-methoxynaphthalen 22, 2,4-dichlorophenyl 18 and quinoline carrying a chromene-3-carboxamide moiety 25 were nearly as active as doxorubicin, while quinoline acrylamides incorporating unsubstituted phenyl 2, p-tolyl 3, 2,4-dienamide 8, 3-nitrophenyl 13, 4-nitrophenyl 14, 3,4-dimethoxyphenyl 16 and chromene 26 exhibited a moderate activity. In addition, quinoline with acetamide 1, 4-hydroxyphenyl 4, 4-dimethylaminophenyl 9, 4-chlorophenyl 11, 3-bromophenyl 20, 4-bromophenyl 21 and 3-thienyl moiety 24 showed less activity than doxorubicin. On the other hand, quinoline having 2-methoxyphenyl 5, 4-methoxyphenyl 6, 4-metho xynaphthalene 23 and chromene-2-carboxamide 28 showed no activity.

A novel series of quinazoline derivatives 2-8, 10-12 were designed and synthesized. Structures of the newly synthesized compounds were confirmed by elemental analyses, IR, 1H and 13C NMR spectral data. All the newly synthesized compounds were evaluated for in vitro cytotoxic activity against the breast cancer cell line MCF-7. Seven of the novel compounds exhibited higher activity than the reference drug doxorubicin. The corresponding compounds 3, 4, 5, 8, 10, 11 and 12 exhibited higher activity with IC50 values from 22.75 to 43.44 μmol L−1, compared to the reference drug doxorubicin with IC50 value of 47.90 μmol L−1. Also, compounds 1, 6, and 9 are nearly as active as doxorubicin with IC50 values of 48.31, 48.90, and 48.91 μmol L−1, respectively, while compounds 2 and 7 exhibited a moderate activity with IC50 values of 50.44 and 52.37 μmol L−1. In addition, compound 13 showed no activity. Cytotoxic screening of the tested copmpounds offered an encouraging framework that may lead to the discovery of potent anti-breast cancer activity.

C20H23N3O5S, monoclinic, P21/c (no. 14), a = 6.7503(2) Å, b = 14.0026(7) Å, c = 21.954(1) Å, β = 96.892(3)°, V = 2060.14(15) Å3, Z = 4, Rgt(F) = 0.0545, wRref(F2) = 0.1192, T = 100 K.

C12H11N5O6, triclinic, P1̅ (no. 2), a = 10.4031(5) Å, b = 11.3191(5) Å, c = 13.2540(6) Å, α = 97.666(2)°, β = 102.252(2)°, γ = 110.182(2)°, V = 1394.73(11) Å3, Z = 4, Rgt(F) = 0.0348, wRref(F2) = 0.1030, T = 100 K, Dcalc = 1.530 mg m−3.

C9H5ClN4, monoclinic, P21/c (no. 14), a = 8.1178(4) Å, b = 7.2367(4) Å, c = 15.2585(8) Å, β = 101.506(2)°, V = 878.36(8) Å3, Z = 4, Rgt(F) = 0.0466, wRref(F2) = 0.1170, T = 100 K.

C11H14N2O3S, orthorhombic, Pbca (no. 61), a = 10.1973(3) Å, b = 9.9487(4) Å, c = 23.1332(8) Å, V = 2346.86(14) Å3, Z = 8, Rgt(F) = 0.0527, wRref(F2) = 0.1407, T = 100 K.

C11H17NO2, monoclinic, P21/c (no. 14), a = 5.9245(2) Å, b = 17.7243(6) Å, c = 10.2915(4) Å, β = 95.352(1)°, V = 1075.97(7) Å3, Z = 4, Rgt(F) = 0.0419, wRref(F2) = 0.116, T = 100(2) K.

A novel series of thiophenes having biologically active sulfonamide 2-11, 3-methylisoxazole 12, 4-methoxybenzo[d] thiazole 13, quinoline 14, 15, benzoylphenylamino 16, and anthracene-9,10-dione 17 moieties were prepared. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. All newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Most of the screened compounds showed cytotoxic activities compared to doxorubicin as a positive control. Compounds 6, 7, 9 and 13 (IC50 values 10.25, 9.70, 9.55 and 9.39 μmol L-1) revealed higher cytotoxic activities than that of doxorubicin (IC50 = 32.00 μmol L-1). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 28.85, 23.48 and 27.51 μmol L-1).

A series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against the Grampositive bacteria Staphyllococcus aureus and Bacillius subtilis and the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, in addition to the fungi organisms, Candida albicans, C. parapsilosis and C. tropicalis. Ethyl 5-(2,5-dimethylthiophen- 3-yl)-1-phenyl-1H-pyrazole-3-carboxylate (21) (MICE.coli = 0.038 μmol mL-1, MICP. aerug. = 0.067 μmol mL-1) is nearly as active as ampicillin (MIC = 0.033 and 0.067 μmol mL-1), respectively. Ethyl 5-(4-bromo-2-chlorophenyl)- 1-phenyl-1H-pyrazole-3-carboxylate (16) (MIC = 0.015 μmol mL-1) is more active than fluconazole (0.020 μmol mL-1) as a reference drug against C. parapsilosis.

C7H10Cl2N2O2, monoclinic, P21/c (no. 14), a = 9.8798(3) Å, b = 13.9285(5) Å, c = 7.3161(3) Å, β = 100.512(3)°, V = 989.88(6) Å3, Z = 4, Rgt(F) = 0.0475, wRref(F2) = 0.1178, T = 296 K.

C13H17NO3, monoclinic, P21/c, a = 7.7486(4) Å, b = 8.5148(3) Å, c = 19.9822(9) Å, β = 100.341(2)°, V = 1296.97(10) Å3, Z = 4, Rgt(F) = 0.0620, wRref(F2) = 0.1814, T = 296 K.