A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: The disclosure of a new antitumor pharmacophore in protoapigenone 1

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 11, 2011, Pages 3427-3430

  Yuan, Qianying ^a   Liu, Ziwei ^a   Xiong, Chaomei ^a   Wu, Liqian ^a   Wang, Jianping ^a   Ruan, Jinlan ^a  

^a HUAZHONG UNIVERSITY OF SCIENCE AND TECHNOLOGY   (China)

Author keywords

4 Hydroxy 2,5 cyclohexadien 1 one; Antitumor activity; In vitro and in vivo screening; Protoapigenone; Synthesis

Indexed keywords

1 HYDROXYCYCLOHEXA 2,5 DIEN 4 ONE; 2 (1 HYDROXY 4 OXOCYCLOHEXA 2,5 DIENYL)PYRAN 4 ONE; 2 (2 BROMOETHYL) 1,3 DIOXOLANE; 2 (2 NITROETHYL) 1,3 DIOXOLANE; 2 (4 HYDROXYPHENYL)PYRONE; ANTINEOPLASTIC AGENT; APIGENIN DERIVATIVE; PROTOAPIGENONE 1; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CANCER INHIBITION; CYTOTOXICITY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; HEMATOLOGIC MALIGNANCY; HEMATOPOIESIS; HUMAN; IC 50; IMMUNOREACTIVITY; LIVER CANCER; NONHUMAN; OVARY CANCER; PANCREAS CANCER; PHARMACOPHORE; PROSTATE CANCER; STRUCTURE ACTIVITY RELATION;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; CYCLOHEXANONES; FEMALE; FLAVONES; HUMANS; INHIBITORY CONCENTRATION 50; MALE; NEOPLASMS;

EID: 79956064228     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.03.108     Document Type: Article

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16. 7 cells/ml. A volume of 0.2 ml of H22 tumor cell suspension was hypodermically injected into the right flank of each mouse. Twenty-four hours after injection of the H22 cells, the mice were randomly divided into four groups, that is, a model group, a compound 1 group, a compound 9 group, a Cyclophosphamide (CTX) group, 10 mice in each group, and with a normal group set as the controls (0.2 ml saline was injected into the right axillary fossa for each mouse of this group). From the second day after inoculation, 1 and 9 dissolved in 10% ethanol solution were administered for seven successive days by intraperitoneal injection (10 ml/kg for each mouse) at daily dose of 10 mg/kg. CTX (10 mg/kg) was used as reference drug. Normal animals and untreated tumor bearing animals were treated with the same volume of 10% ethanol solution. The mice were killed at day nine. The tumors, thymus, and spleen were separated and weighed, the blood sample was taken for count of WBC and the femurs were dissected and marrow cells flushed from the bone. The tumor inhibition rate was calculated: (the tumor weight of the model group - the tumor weight of the treatment group)/the tumor weight of the model group × 100% and the thymus index and the spleen index were calculated: The thymus index = the thymus weight (mg)/body weight (g); while the spleen index = the spleen weight (mg)/body weight (g). Numbers of nucleated cells of the bone marrow were determined using a Coulter Counter. The counts of granulocytic or erythroid cells per femur were performed on marrow smears stained with the May-Grünwald-Giemsa method.